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Rimonabant (SR141716)

中文名稱：利莫那班

Rimonabant (SR141716)是一個大腦中心大麻素受體（CB1）特異性口服拮抗劑。在hCB1轉染HEK293細胞中IC50濃度為13.6 nM，EC50濃度為17.3 nM。Rimonabant也是一種acyl CoA:cholesterol acyltransferases(ACAT) 1和2的雙重抑制劑并且可抑制分支桿菌的MmpL3。

Rimonabant (SR141716) Chemical Structure

Rimonabant (SR141716) Chemical Structure

CAS: 168273-06-1

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 990.19 現(xiàn)貨
10mg 729.08 現(xiàn)貨
25mg 1373.02 現(xiàn)貨
50mg 2214.44 現(xiàn)貨
100mg 3016.81 現(xiàn)貨
1g 9990 現(xiàn)貨
更大包裝 有超大折扣

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Rimonabant (SR141716)相關產(chǎn)品

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
CHO Function assay > 0.1 nM 1 hr Inverse agonist activity at human recombinant CB1 receptor transfected in CHO cells assessed as reduction of [35S]GTPgammaS binding at > 0.1 nM after 1 hr by liquid scintillation spectrometry 23357307
N1E-115 Function assay 1 uM 5 mins Inverse agonist activity at CB1 receptor in mouse N1E-115 cells assessed as inhibition of WIN 55,212-2-induced ERK1/2 phosphorylation at 1 uM treated 5 mins prior to WIN 55,212-2 challenge by Western blot analysis 23357307
HEK293 Function assay 10 uM Intrinsic activity at human recombinant CB1R expressed in HEK293 cells assessed as Eu-GTP binding at 10 uM relative to basal level 19530697
CHOK1 Function assay 10 mins Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay, Ki=0.0016μM 19351113
CHO Function assay 60 mins Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins, EC50=0.00011μM 20047779
CHO Function assay 3 hrs Displacement of [3H]CP-55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.00074μM 20047779
CHO Function assay 10 mins Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells coexpressing Galpha15/16 assessed as inhibition of CP-55940-induced Ca2+ release after 10 mins by micro plate reader, IC50=0.0032μM 20047779
CHO Function assay 3 hrs Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.126μM 20047779
CHO-K1 Function assay 1 hr Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting, IC50=1.76μM 20673729
CHO Function assay 1 hr Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting, IC50=1.98μM 21741835
HEK293 Function assay 5 mins Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay, IC50=2.79μM 21741835
CHO Function assay 90 mins Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation counting, Ki=0.00073μM 21962575
CHO Function assay 2 hrs Displacement of [3H]CP55,940 from human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.0126μM 22916707
CHO Function assay 2 hrs Displacement of [3H]CP55,940 from human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.9μM 22916707
CHO Function assay 1 hr Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cells incubated for 1 hr, Ki=0.0106μM 23072339
HEK Function assay 1 hr Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis, EC50=0.0015μM 24175572
CHOK1 Function assay 1 hr Displacement of [3H]CP55940 from human CB1 receptor expressed in CHOK1 cells after 1 hr by liquid scintillation counting analysis, Ki=0.0059μM 24175572
CHO Function assay 45 mins Antagonist activity at human CB1 receptor stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=0.013μM 24445310
CHO Function assay 45 mins Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=9.8μM 24445310
CHO-K1 Function assay 10 mins Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting, Ki=0.0016μM 24900484
HEK293 Function assay 60 mins Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting, Ki=0.0018μM 24900484
CHO-K1 Function assay 60 mins Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells after 60 mins by beta counting, Ki=0.522μM 24900484
CHO Function assay 2 hrs Displacement of [3H]CP55,940 from recombinant human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.0126μM 24900561
CHO Function assay 2 hrs Displacement of [3H]CP55,940 from recombinant human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.9μM 24900561
CHO Function assay 90 mins Agonist activity at GPR55 (unknown origin) expressed in CHO cells assessed as inhibition of LPI-induced beta-arrestin translocation after 90 mins by luminescence assay, EC50=2.01μM 24900561
Sf9 Function assay 20 mins Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05μM 25096297
Sf9 Function assay 20 mins Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05012μM 25096297
HEK293 Function assay 90 mins Displacement of [3H]-CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.012μM 26756097
HEK293 Function assay 90 mins Displacement of [3H]-CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.79μM 26756097
CHO Function assay 90 secs Inverse agonist activity at human CB1 receptor expressed in CHO cells assessed as increase in intracellular calcium mobilization after 90 secs by Calcein-4 AM-staining based FLIPR assay, EC50=0.005μM 26827137
CHOK1 Function assay 90 mins Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment after 90 mins by chemiluminescent assay, EC50=0.015μM 29939744
HEK293 Function assay 90 secs Inverse agonist activity at human CB1 receptor expressed in HEK293 cells co-expressing Galphaq16 assessed as inhibition of calcium mobilization after 90 secs by calcein-4 AAM dye-based FLIPR assay, EC50=0.586μM 30077609
HEK293 Function assay 30 mins Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay, EC50=0.0041μM 30339387
CHO Function assay Antagonistic activity against cannabinoid receptor 1 measured by CP-55940 induced arachnoid acid release in CHO cells, Kd=0.002512μM 16140010
CHO Function assay Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells, Ki=0.0054μM 15801840
CHO Function assay In vitro displacement of CP-55940 binding to human CB2 receptor expressed in CHO cells, Ki=1.58μM 15771428
CHO Function assay In vitro displacement of CP-55940 binding to human CB1 receptor expressed in CHO cells, Ki=0.025μM 15771428
CHO Function assay In vitro cannabinoid receptor 1 antagonism of [3H]arachidonic acid release by CHO cells, Kd=0.002512μM 15771428
CHO Function assay Inhibitory concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells, IC50=0.006μM 15713403
CHO Function assay Affinity to displace CP-55940 binding from Cannabinoid receptor 2 of human expressed in CHO cells, Ki=1.58μM 14736243
CHO Function assay Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells, Ki=0.025μM 14736243
CHO Function assay Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells, Kd=0.002512μM 14736243
CHO cells Function assay Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes, Ki=8.9 nM 10465552
CHO Function assay Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 1, Ki=0.025μM 16140010
CHO Function assay Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 2, Ki=1.58μM 16140010
CHOK1 Function assay Functional activity at human CB1 receptor transfected in CHOK1 cells by [35SGTP]gammaS assay, Ki=0.001μM 16263283
HEK293 Function assay Displacement of [3H]SR-141716 from human CB1 receptor transfected in HEK293 cells, Ki=0.0021μM 16263283
CHO Function assay Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0054μM 16279809
HEK293 Function assay Displacement of [3H]SR-141716 from human CB1 receptor expressed in HEK293 cells, Kd=0.0018μM 17004712
HEK293 Function assay Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0071μM 17004712
HEK293 Function assay Displacement of [3H]WIN-55212-2 from human CB1 receptor expressed in HEK293 cells, Ki=0.018μM 17004712
CHO Function assay Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells, IC50=0.0061μM 17181138
CHO Function assay Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells, IC50=0.6μM 17181138
CHO Function assay Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells, IC50=0.0061μM 17293109
CHO Function assay Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells, IC50=0.6033μM 17293109
HEK293 Function assay Displacement of [3H]CP-559440 from human CB1 receptor expressed in HEK293 cells, Ki=0.0011μM 17383180
HEK293 Function assay Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.016μM 17942307
HEK293 Function assay Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=1.64μM 17942307
HEK293 Function assay Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.047μM 17979261
CHOK1 Function assay Displacement of [3H]WIN-552122 from human recombinant CB2 receptor expressed in CHOK1 cells, Ki=1.99μM 17979261
HEK293 Function assay Displacement of radioligand from human CB1 receptor expressed in HEK293 cells, Ki=0.0018μM 18083560
HEK293 EBNA Function assay Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay, EC50=0.004μM 18083560
HEK293 Function assay Displacement of radioligand from human CB2 receptor expressed in HEK293 cells, Ki=0.554μM 18083560
CHOK1 Function assay Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay, IC50=0.12μM 18243711
CHOK1 Function assay Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM 18243711
HEK Function assay Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM 18293908
HEK Function assay Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM 18293908
HEK293 Function assay Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells, Ki=0.006μM 18335976
CHO Function assay Displacement of [3H]WIN-55212-2 from human cannabinoid CB2 receptor expressed in CHO cells, IC50=1.76μM 18337096
CHO Function assay Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM 18342403
CHO Function assay Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, Ki=1.58μM 18342403
HEK293 Function assay Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0024μM 18363352
CHO Function assay Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=0.56μM 18363352
SF9 Function assay Antagonist activity at rat CB1 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00031μM 18448340
SF9 Function assay Antagonist activity at human CB1 receptor expressed in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00043μM 18448340
SF9 Function assay Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS level, IC50=0.00135μM 18448340
SF9 Function assay Antagonist activity at human CB2 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.815μM 18448340
HEK293 Function assay Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.04μM 18511157
CHO-K1 Function assay Displacement of [3H]SR141716 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.00118μM 18512901
HEK293 Function assay Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated [35S]GTPgammaS binding, Kd=0.00257μM 18512901
HEK293 Function assay Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM 18512901
CHO-K1 Function assay Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM 18512901
HEK Function assay Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.008μM 18579386
HEK Function assay Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM 18579386
HEK293 Function assay Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.012μM 18680276
HEK293 Function assay Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, Ki=0.79μM 18680276
HEK293 Function assay Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM 18712856
HEK293 Function assay Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM 18712856
HEK293 Function assay Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=1.9398μM 18712856
HEK293 Function assay Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as decrease in [35S]gammaGTP binding relative to control 18712856
CHO Function assay Antagonist activity at human CB1 receptor in CHO cells assessed as GTPgammaS binding, Kb=0.000698μM 18800770
CHOK1 Function assay Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM 18954042
CHO Function assay Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, IC50=1.76μM 19022666
HEK293 Function assay Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=0.0019μM 19095444
HEK293 Function assay Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM 19095444
HEK293 Function assay Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM 19095444
CHO-K1 Function assay Antagonist activity against human CB1 receptor expressed in CHO-K1 cells by [35S]GTPgamma binding assay, Ki=0.00019μM 19102698
HEK293 Function assay Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells, Ki=0.0009μM 19102698
CHOK1 Function assay Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM 19269817
CHOK1 Function assay Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=0.24μM 19328683
CHOK1 Function assay Antagonist activity at human cannabinoid CB2 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=31.21μM 19328683
HEK293 Function assay Displacement of [3H]SR141716 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.001995μM 19338356
HEK293 Function assay Displacement of [3H]SR141716 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=0.39811μM 19338356
HEK293 Function assay Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.0019μM 19520572
HEK293 Function assay Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells, IC50=0.0132μM 19530697
HEK293 Function assay Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding, EC50=0.0157μM 19530697
HEK293 Function assay Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells, IC50=1.6311μM 19530697
HEK Function assay Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM 19595596
HEK Function assay Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM 19595596
CHO-K1 Function assay Antagonist activity at human CB1 receptor transfected in CHO-K1cells by GTPgamma[35S] binding assay, Ki=0.0016μM 19683918
CHO Function assay Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.0925μM 19850473
CHOK1 Function assay Displacement of [3H]WIN-552122 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM 19850473
CHO-K1 Function assay Antagonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, IC50=0.0045μM 19954978
CHO-K1 Function assay Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay, IC50=0.0029μM 20015647
CHO-K1 Function assay Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced GTPgammaS binding, IC50=0.0045μM 20015647
COS7 Function assay Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS7 cells, IC50=0.0051μM 20015647
CHO Function assay Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.108μM 20045337
CHO Function assay Antagonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of CP-55940-induced [3H]arachidonic acid release, Kd=0.002512μM 20363132
CHO Function assay Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM 20363132
CHO Function assay Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=1.58μM 20363132
HEK Function assay Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells, Ki=0.012μM 20718492
HEK Function assay Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK cells, Ki=0.79μM 20718492
CHO Function assay Agonist activity at human CB1 receptor expressed in CHO cells co-expressing Galpha16 protein assessed as mobilization of intracellular calcium, Ke=0.0011μM 20845959
HEK293 Function assay Displacement of [3H]SR141716 from human CB1 receptor expressed in HEK293 cells, Ki=0.00118μM 20845959
HEK293 Function assay Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM 20845959
CHOK1 Function assay Displacement of [3H]CP55940 from human CB2 receptor expressed in CHOK1 cells, Ki=0.313μM 20845959
HEK Function assay Displacement of [3H]CP-55,940 from recombinant human CB1 receptor transfected in HEK cells, Ki=0.012μM 20943290
HEK Function assay Displacement of [3H]CP-55,940 from recombinant human CB2 receptor transfected in HEK cells, Ki=0.79μM 20943290
CHO Function assay Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0009333μM 21334892
Sf9 Function assay Displacement of [3H]CP55940 from human recombinant CB2 receptor expressed in Sf9 cells, Ki=0.85114μM 21334892
CHO Function assay Antagonist activity at CB1 receptor transfected in CHO cells expressing apoaequorin as a reporter for G-protein-coupled receptor-mediated calcium signaling by bioluminescence assay, IC50=0.004μM 21376588
HEK293 Function assay Noncompetitive inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells by Dixon plot, Ki=1.4μM 21511945
HEK293 Function assay Noncompetitive inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells by Dixon plot, Ki=4μM 21511945
HEK293 Function assay Induction of MRP2-mediated E2-17betaG transport in human MRP2 expressing HEK293 cells in presence of 2 uM E2-17betaG 21511945
HEK293 Function assay Inhibition of MRP3-mediated E2-17betaG transport in human MRP3 expressing HEK293 cells in presence of 15 uM E2-17betaG 21511945
HEK293 Function assay Inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG 21511945
HEK293 Function assay Inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG 21511945
HEK Function assay Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM 21702498
HEK Function assay Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM 21702498
CHO-K1 Function assay Antagonist activity at human CB1 receptor expressed in CHO-K1 cells co-expressing Galphaq16 assessed as inhibition of CP55940-induced intracellular calcium mobilization by fluorometry, Ke=0.0011μM 22372835
CHO-K1 Function assay Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.0062μM 22372835
CHO-K1 Function assay Displacement of [3H]CP55940 from CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM 22372835
HEK Function assay Displacement of [3H]CP-55,940 from human recombinant CB1 receptor transfected in HEK cells, Ki=0.012μM 22548457
HEK Function assay Displacement of [3H]CP-55,940 from human recombinant CB2 receptor transfected in HEK cells, Ki=0.79μM 22548457
CHO Function assay Inverse agonist activity against CB1 receptor expressed in human CHO cells assessed as effect on forskolin-stimulated cAMP level, IC50=0.051μM 22959249
CHO Function assay Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay, IC50=10.1μM 23679955
RD-HGA16 Function assay Antagonist activity at CB1-OX1 heterodimer (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of orexin A-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.001μM 24944734
RD-HGA16 Function assay Antagonist activity at CB1 receptor (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of CP55940-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.0011μM 24944734
CHO Function assay Antagonist activity against CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=0.0135μM 26151231
CHO Function assay Antagonist activity against CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=9.1μM 26151231
HEK293 Function assay Immediate antagonist/Inverse agonist activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as reversal of 1 uM CP55,940-induced inhibition of 5 uM forskolin-induced cAMP accumulation by kinetic cAMP assay 26203658
CHO-K1 Function assay Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP55940-induced intracellular calcium mobilization by Calcein-4 AM-staining based FLIPR assay, Ke=0.0011μM 26827137
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
HEK293 Function assay Antagonist activity at human CB1 receptor expressed in HEK293 cells by GTPgammaS binding assay, Ke=0.0002μM 30077609
CHO Function assay Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells by radioligand binding assay, Ki=0.143μM 31609608
CHO Function assay Agonist activity at human GPR55 expressed in CHO cells assessed as induction of LPI-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=2.01μM ChEMBL
CHO Function assay Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=10.1μM ChEMBL
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生物活性

產(chǎn)品描述 Rimonabant (SR141716)是一個大腦中心大麻素受體（CB1）特異性口服拮抗劑。在hCB1轉染HEK293細胞中IC50濃度為13.6 nM，EC50濃度為17.3 nM。Rimonabant也是一種acyl CoA:cholesterol acyltransferases(ACAT) 1和2的雙重抑制劑并且可抑制分支桿菌的MmpL3。
特性 有效誘導體重降低，并改善心血管代謝危險因素，然而由于引起嚴重的抑郁癥和焦慮在2009年撤回。
靶點
ACAT1 [2] ACAT2 [2] MmpL3 [7] hCB1 [1]
(Cell-free assay)		 hCB2 [1]
(Cell-free assay)
13.6 nM 1.64 μM
體外研究(In Vitro)
體外研究活性

Rimonabant劑量依賴性降低Raw264.7巨噬細胞和離體腹膜巨噬細胞中ACAT活性，IC50為2.9 μM。Rimonabant以近似的效能抑制完整CHO-ACAT1和CHO-ACAT2細胞以及無細胞試驗中ACAT活性，對CHO-ACAT1和 CHO-ACAT2的IC50分別為1.5 μM和2.2 μM。與ACAT抑制一致，Rimonabant治療阻斷巨噬細胞中ACAT相關過程，氧甾醇誘導的細胞凋亡和乙?；疞DL誘導的泡沫細胞形成。[2] Rimonabant顯著減少細胞生長，并誘導人結腸直腸癌細胞(DLD-1，CaCo-2和SW620)的死亡。Rimonabant能夠改變所有測試細胞系中細胞周期分布。特別是，Rimonabant引起DLD-1細胞中細胞周期阻滯，而不誘導細胞凋亡或壞死。[4]
激酶實驗 配體結合試驗
將人CB1和CB2穩(wěn)定轉染的HEK 293細胞和細胞膜純化。0.2-8 μg純化的細胞膜與0.75 nM [3H] CP55,940和Rimonabant在孵育液(50 mM Tris-HCl，5 mM MgCl2，1 mM EDTA，0.3%BSA，pH 7.4)中培育。非特異性結合在1 μM CP55,940存在下定義。反應在30 °C下，Multiscreen中培育1.5小時。反應通過多重過濾終止，并且用冰預冷的洗滌緩沖液(50mM Tris，pH 7.4，0.25% BSA)清洗4次。過濾器上的放射性結合通過Topcount測量。IC50定義為抑制50%[3H] CP55,940結合時Rimonabant的濃度，并通過非線性回歸計算。
細胞實驗 細胞系 Raw 264.7細胞
濃度 0,1,4 μM
孵育時間 17小時
方法

Raw 264.7細胞(2×106/孔)在12孔板中用PBS漂洗，培養(yǎng)基用不同量Rimonabant增補，1小時后用7-酮基膽固醇(7KC)增補。所有孔加入等量的載體。培育16小時后，caspase-3和caspase 3樣活性使用熒光底物(Ac-DEVD-AFC)和配備酶標儀的分光光度計測定。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot CD44 / Lgr5 / CD133 / EpCAM β-catenin p-LRP6 / LRP6 / Lgr5 29354056
Immunofluorescence β-catenin Lgr5 29354056
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Rimonabant腹腔內(nèi)給藥或口服給藥有效且劑量依賴性拮抗大麻素受體激動劑的經(jīng)典藥理學和行為作用。[3]在氧化偶氮甲烷誘發(fā)的結腸癌模型中，結腸直腸癌發(fā)生之前，Rimonabant顯著減少異常隱窩病灶(ACF)的形成。[4] Rimonabant (10 mg/kg，強飼)對3個月大雄性肥胖Zucker大鼠喂食2周作為葡萄糖耐量降低模型，對6個月大雄性肥胖Zucker大鼠喂食10周作為代謝綜合征模型。相對于瘦的Zucker大鼠，RANTES (正常T細胞表達和分泌的活性調節(jié)蛋白)和MCP-1 (單核細胞趨化蛋白-1)血清水平在肥胖Zucker大鼠體內(nèi)增加，而在Rimonabant長期治療下顯著降低，這表明代謝綜合征大鼠的體重增加。相對于瘦的Zucker大鼠，Neutrophils和單核細胞在年老和幼小的肥胖Zucker大鼠中顯著增加，但是被Rimonabant降低。相對于瘦的Zucker大鼠，血小板結合的纖維蛋白原在兩個年齡段肥胖Zucker大鼠中顯著增加，但是被Rimonabant減少。來自肥胖大鼠的血小板對凝血酶誘導的聚集更敏感，并粘附在纖維蛋白原上，這都會被Rimonabant治療減弱。[5]
動物實驗 Animal Models 雄性小鼠和雄性大鼠
Dosages 20 ml/kg (小鼠) 和 5 ml/kg (大鼠)
Administration WIN55212-2靜脈注射之前，Rimonabant 通過腹腔注射(30 分鐘)或口服(1 小時)給藥
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00750347 Completed
Pain
University Hospital Clermont-Ferrand
 September 2008 Phase 1
NCT00656487 Completed
Cannabis Dependence|Cannabis Withdrawal
The Scripps Research Institute|National Institute on Drug Abuse (NIDA)
 April 30 2008 Phase 2
NCT00546325 Completed
Diabetes Mellitus Type 2
Sanofi
 October 2007 Phase 3
NCT00525681 Completed
Renal Transplantation
University of Oslo School of Pharmacy
 September 2007 Phase 4
NCT00584389 Terminated
Obesity
University of Surrey|European Foundation for the Study of Diabetes|Royal Surrey County Hospital NHS Foundation Trust
 July 2007 Phase 4
NCT01041170 Completed
Cannabis|Dependence
National Institute on Drug Abuse (NIDA)|National Institutes of Health Clinical Center (CC)
 April 16 2006 Phase 1

化學信息&溶解度

分子量 463.79 分子式

C22H21Cl3N4O
CAS號 168273-06-1 SDF Download Rimonabant (SR141716) SDF
Smiles CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)Cl
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 92 mg/mL ( (198.36 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 50 mg/mL (107.8 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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