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  2. GPCR/G Protein Neuronal Signaling Anti-infection
  3. Cannabinoid Receptor Bacterial
  4. Rimonabant Hydrochloride

Rimonabant Hydrochloride  (Synonyms: 鹽酸利莫那班; SR 141716A Hydrochloride)

目錄號(hào): HY-14137 純度: 99.95%
COA 產(chǎn)品使用指南 技術(shù)支持

Rimonabant Hydrochloride (SR 141716A Hydrochloride) 是中心大麻素受體 1 (CB1) 高效的、選擇性的反向激動(dòng)劑， Ki 值為1.8 nM。Rimonabant Hydrochloride (SR 141716A Hydrochloride) 也能夠抑制分枝桿菌膜蛋白3 (MMPL3)。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Rimonabant Hydrochloride Chemical Structure

Rimonabant Hydrochloride Chemical Structure

CAS No. : 158681-13-1

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥638
In-stock
1 mg ￥165
In-stock
5 mg ￥331
In-stock
10 mg ￥530
In-stock
50 mg ￥1825
In-stock
100 mg ￥2550
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Rimonabant Hydrochloride:

查看 Cannabinoid Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Rimonabant Hydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant Hydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

IC50 & Target[1]

CB1

1.8 nM (Ki)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
BV-2 IC50
16.17 μM
Compound: Rimonabant
Inhibition of LPS-induced NO production in mouse BV-2 cells incubated for 24 hrs by Griess reagent based method
Inhibition of LPS-induced NO production in mouse BV-2 cells incubated for 24 hrs by Griess reagent based method
[PMID: 36371018]
CHO IC50
0.004 μM
Compound: Rimonabant
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
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
[PMID: 21376588]
CHO IC50
0.0135 μM
Compound: 2, SR141716A
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
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
[PMID: 26151231]
CHO EC50
0.11 nM
Compound: Rimonabant
Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 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
[PMID: 20047779]
CHO IC50
1.98 μM
Compound: 1
Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting
Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting
[PMID: 21741835]
CHO EC50
10.1 μM
Compound: 5
Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method
Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method
10.1039/C3MD00394A
CHO IC50
10.1 μM
Compound: 1
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
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
[PMID: 23679955]
CHO IC50
108 nM
Compound: 1
Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay
Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay
[PMID: 20045337]
CHO IC50
13 nM
Compound: SR141716A, Rimonabant
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
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
[PMID: 24445310]
CHO EC50
2.01 μM
Compound: 6
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
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
[PMID: 24900561]
CHO EC50
2.01 μM
Compound: 5
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
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
10.1039/C3MD00394A
CHO IC50
3.2 nM
Compound: Rimonabant
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
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
[PMID: 20047779]
CHO EC50
5 nM
Compound: 1; SR141716A
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
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
[PMID: 26827137]
CHO IC50
9.1 μM
Compound: 2, SR141716A
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
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
[PMID: 26151231]
CHO IC50
92.5 nM
Compound: Rimonabant
Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay
Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay
[PMID: 19850473]
CHO IC50
9800 nM
Compound: SR141716A, Rimonabant
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
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
[PMID: 24445310]
CHO-K1 IC50
> 1000 nM
Compound: Rimonabant
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells by liquid scintillation counting
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells by liquid scintillation counting
[PMID: 19128970]
CHO-K1 IC50
120 nM
Compound: 1, SR-141716,rimonabant
Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay
Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay
[PMID: 18243711]
CHO-K1 IC50
1760 nM
Compound: 1
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting
[PMID: 20673729]
CHO-K1 IC50
1760 nM
Compound: SR-141716
Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry
Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry
[PMID: 19269817]
CHO-K1 IC50
1760 nM
Compound: 1, rimonabant, SR-141716
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry
[PMID: 18954042]
CHO-K1 IC50
2.9 nM
Compound: Rimonabant
Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay
Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay
[PMID: 20015647]
HEK293 EC50
1.5 nM
Compound: 1, SR141716A, Zimulti
Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis
Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis
[PMID: 24175572]
HEK293 IC50
2.79 μM
Compound: 1
Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay
Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay
[PMID: 21741835]
HEK293 IC50
2.8 nM
Compound: SR141716
Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method
Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method
[PMID: 31596583]
HEK293-EBNA EC50
4 nM
Compound: 1, rimonabant
Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay
Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay
[PMID: 18083560]
Sf9 EC50
0.05 μM
Compound: Rimonabant
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
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
[PMID: 25096297]
體外研究
(In Vitro)

Rimonabant 可以抑制 Mtb 的生長(zhǎng)，MIC 為 54 μM。MmpL3 是抗結(jié)核靶標(biāo)，是 Rimonabant Hydrochloride 的直接靶標(biāo)[2]。
Rimonabant Hydrochloride 本身 (10-12-10-3 M，12 個(gè)濃度組) 以濃度依賴性方式抑制 [35S]GTPgS 與人皮層膜的基礎(chǔ)結(jié)合，-log IC50 為 4.7±0.2 (IC50 = 20 μM)，最大抑制率為 48±2%[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

將 Rimonabant (10 mg/kg 灌胃法) 將 3 個(gè)月大的雄性肥胖 Zucker 大鼠作為葡萄糖耐量受損模型喂食 2 周，將 6 個(gè)月大的雄性肥胖 Zucker 大鼠作為代謝綜合征模型喂食 10 周。 RANTES 和 MCP-1 血清水平在肥胖和瘦 Zucker 大鼠中增加，并且通過(guò)長(zhǎng)期使用 Rimonabant 治療顯著降低，這減緩了患有代謝綜合征的大鼠的體重增加。中性粒細(xì)胞和單核細(xì)胞在年輕和年老的肥胖與瘦 Zucker 大鼠中顯著增加，而被 Rimonabant 降低。 血小板結(jié)合纖維蛋白原在兩個(gè)年齡段的肥胖和瘦 Zucker 大鼠中顯著增強(qiáng)，并且被 Rimonabant 降低[1]。
Rimonabant (每天 20 毫克) 表現(xiàn)出許多心臟代謝危險(xiǎn)因素的顯著減少[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

500.25

Formula

C22H22Cl4N4O
CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

鹽酸利莫那班
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 33.33 mg/mL (66.63 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.9990 mL 9.9950 mL 19.9900 mL
5 mM 0.3998 mL 1.9990 mL 3.9980 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.00 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.00 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.95%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9990 mL 9.9950 mL 19.9900 mL 49.9750 mL
5 mM 0.3998 mL 1.9990 mL 3.9980 mL 9.9950 mL
10 mM 0.1999 mL 0.9995 mL 1.9990 mL 4.9975 mL
15 mM 0.1333 mL 0.6663 mL 1.3327 mL 3.3317 mL
20 mM 0.1000 mL 0.4998 mL 0.9995 mL 2.4988 mL
25 mM 0.0800 mL 0.3998 mL 0.7996 mL 1.9990 mL
30 mM 0.0666 mL 0.3332 mL 0.6663 mL 1.6658 mL
40 mM 0.0500 mL 0.2499 mL 0.4998 mL 1.2494 mL
50 mM 0.0400 mL 0.1999 mL 0.3998 mL 0.9995 mL
60 mM 0.0333 mL 0.1666 mL 0.3332 mL 0.8329 mL
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Bulk Inquiry

Inquiry Information

產(chǎn)品名稱：
Rimonabant Hydrochloride
目錄號(hào)：
HY-14137
需求量：