BAY 11-7082

別名: BAY 11-7821

目錄號(hào)：S2913 Purity: 99.98%

BAY 11-7082 (BAY 11-7821)是一種 NF-κB 抑制劑，抑制TNFα誘導(dǎo)的 IκBα 磷酸化，在腫瘤細(xì)胞中IC50為10 μM。BAY 11-7082 可抑制 ubiquitin-specific protease USP7 和 USP21，對(duì)應(yīng)的IC50值分別為0.19 μM和0.96 μM。BAY 11-7082 在胃癌細(xì)胞中可誘導(dǎo)凋亡和S期阻滯。

BAY 11-7082 Chemical Structure

CAS: 19542-67-7

規(guī)格	價(jià)格	庫(kù)存
10mg	738.58	現(xiàn)貨
50mg	2223.41	現(xiàn)貨
1g	16298.1	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.98%

99.98

BAY 11-7082相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	IκB IKK	點(diǎn)擊展開
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相關(guān)化合物庫(kù)	FDA藥物庫(kù) 免疫/炎癥分子化合物庫(kù) 小分子免疫腫瘤化合物庫(kù) NF-κB信號(hào)通路庫(kù) FDA抗癌藥物庫(kù)	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
SP6.5	Growth Inhibition Assay	2.5-20 μM	24 h?	IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
OM431	Function Assay	5 μM	2 h	decreases?translocation of p65 in the nucleus?	23443086
OCM1	Function Assay	5 μM	2 h	decreases?translocation of p65 in the nucleus?	23443086
VUP	Function Assay	5 μM	2 h	decreases?translocation of p65 in the nucleus?	23443086
SP6.5	Function Assay	5 μM	2 h	decreases?translocation of p65 in the nucleus?	23443086
BAFs	Function Assay	0.5/1?μM	24 h	inhibits TNFα/DEX induced CYP19A1?transcripts	23485457
KMS-12-BM	Apoptosis Assay	30 μM	3 h	induces MM cell death involves necrosis	23527154
MM.1S	Apoptosis Assay	30 μM	3 h	induces MM cell death involves necrosis	23527154
HT29	Function Assay	10/30/100 μM	1 h	inhibits TNF-induced phosphorylation and degradation of IκBα	23527154
HT29	Function Assay	10/30/100 μM	1 h	inhibites both TWEAK-induced p100 processing	23527154
HUVEC	Function Assay	10?μM	0.5 h	counteractes the loss of Tie2 mRNA	23563632
RAW 264?	Function Assay	0.2-5 μM	30/60/90 min	inhibits the phosphatase activity of PTP1B?	23578302
AM	Growth Inhibition Assay	5 μM	4/8 d	reduces the viability of intracellular?MTB	23634218
MDM	Growth Inhibition Assay	5 μM	4/8 d	reduces the viability of intracellular?MTB	23634218
THP-1?	Growth Inhibition Assay	5 μM	4/8 d	reduces the viability of intracellular?MTB	23634218
THP-1	Function Assay	5 μM	1 h	inhibits MTB-induced NFκB activation	23634218
HepG2	Function Assay	0.3/1/3 μM	48 h	reduces IL6-induced PON1 expression	23791833
HBE?	Function Assay	10μM	3h	abolishes the increases of IL-6 expression induced by CSE	23824089
HGC-27?	Apoptosis Assay	7.5/15/30 μM	6 h	induces apoptosis in a time- and dose-dependent manner	23846545
MGC80-3	Function Assay	7.5/15/30 μM	6 h	induces the dephosphorylation and up-regulation of IκBα	23846545
HGC-27?	Function Assay	7.5/15/30 μM	6 h	induces the dephosphorylation and up-regulation of IκBα	23846545
MGC80-3	Growth Inhibition Assay	10/20/30 μM	6/24 h	suppresses cell viability significantly	23846545
AGS	Growth Inhibition Assay	10/20/30 μM	6/24 h	suppresses cell viability significantly	23846545
NCI-N87	Growth Inhibition Assay	10/20/30 μM	6/24 h	suppresses cell viability significantly	23846545
A549	Apoptosis Assay	1?μM	48 h	reduces the cell death induced by combined stimulation	23900080
A549	Function Assay	1?μM	48 h	enhances the up-regulation of IκB and subsequent decrease in Bax expression induced by combined stimulation	23900080
THP-1?	Function Assay	10?μM	1?h	abolishes the effect of rHSP27 on SR-A mRNA	23939398
PC-3	Function Assay	2.5/5/10 μM	0.5 h	blocks IGF-II-induced STS mRNA expression?	24055520
iNKT	Function Assay	10/100 μM	0.5 h	inhibits the induction of A2AR mRNA and other factor	24124453
IVD?	Function Assay	10?μM	3 d	abrogates TNF-α–induced up-regulation of ADAMTS-4 and ADAMTS-5?	24176808
IVD?	Function Assay	10?μM	3 d	reverses TNF-α–mediated suppression of the disc matrix macromolecules aggrecan and collagen II	24176808
A549RT-eto	Function Assay	10?μM	24 h	decreases the expression levels of NF-κB and P-gp?	24220725
A549RT-eto	Apoptosis Assay	10?μM	24 h	accelerates F14 extract-mediated apoptosis combined treatment with F14	24220725
WPs	Function Assay	25 μM	5 min	suppresses ATP and vWF secretion	24331207
DSCs?	Function Assay	2.5 μM	0.5 h	reverses the enhancement of CCL2/CCR2 expression of DSCs induced by IL-33	24344240
OVCXCR2	Function Assay	2 μM	48 h	blocks the CXCL1-induced cell invasion	24376747
SKCXCR2?	Function Assay	2 μM	48 h	blocks the CXCL1-induced cell invasion	24376747
SKCXCR2?	Growth Inhibition Assay	2 μM	48 h	decreases cell proliferation significantly	24376747
THP-1?	Function Assay	0.1/1?μM	0.5 h	abrogates TNF-α secretion as well as the increased secretion of IL-6 and IL-1β	24378536
A549RT-eto	Apoptosis Assay	10?μM	24 h	accelerates FERO-mediated apoptosis	24535083
HUVEC	Function Assay	20 μM	0.5 h	prevents the induction of EAM expression	24551209
A549	Function Assay	10 μM	1?h	inhibits the increase of phospho-IκBα in PA103-infected cultures?	24612488
HeLa?	Function Assay	5?μM	24 h	reduces the activity of TNF-α promoter?	24657783
HUVECs	Function Assay	3-30 μM	1 h	reduces the expression of miR-146a in a dose-dependent manner	24863965
macrophages	Function Assay	5 μM	3 h	partially blocks YPFS-induced expression of iNOS and COX-2?	24967898
RAW 264.7	Function Assay	5?μM	1 h	inhibits TNF-α and IL-12 p40 production	25019567
A549?	Function Assay	10?μM	12 h	suppresses Dvl-3 induced activation of p65	25156800
HMECs	Function Assay	5?μM	2 h	abolishes TNF-α-induced VCAM-1 expression?	25193116
HCT116	Function Assay	5 μM	2 h	attenuates silymarin-induced downregulation of cyclin D1	25479723
ARPE-19	Function Assay	1 μM	0.5 h	suppresses TG-induced?IL-8?promoter activation	25593029
SiHa?	Function Assay	10?μM	1.5 h	abolishes BPA induced up regulation of FN and MMP-9?	25797437
HeLa	Function Assay	10?μM	1.5 h	abolishes BPA induced up regulation of FN and MMP-9?	25797437
VUP	Growth Inhibition Assay	2.5-20 μM	24 h?	IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
OCM1	Growth Inhibition Assay	2.5-20 μM	24 h?	IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
OM431	Growth Inhibition Assay	2.5-20 μM	24 h?	IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
SP6.5	Apoptosis Assay	5 μM	24 h?	induces apoptosis?	23443086
VUP	Apoptosis Assay	5 μM	24 h?	induces apoptosis?	23443086
OCM1	Apoptosis Assay	5 μM	24 h?	induces apoptosis?	23443086
OM431	Apoptosis Assay	5 μM	24 h?	induces apoptosis?	23443086
SP6.5	Function Assay	5 μM	12 h	reduces the migration?	23443086
VUP	Function Assay	5 μM	12 h	reduces the migration?	23443086
OCM1	Function Assay	5 μM	12 h	reduces the migration?	23443086
OM431	Function Assay	5 μM	12 h	reduces the migration?	23443086
HBL-1?	Growth Inhibition Assay	3?μM	24/48/72 h	slows cell growth modestly	23441730
RAW 264.7	Function Assay	2-15 μM	1 h	suppresses the activation of IKK family members	23441730
IL-1R?	Function Assay	2-15 μM	1 h	suppresses the activation of IKK family members	23441730
RAW 264.7	Function Assay	15 μM	1 h	suppresses the activation of and JNK	23441730
IL-1R?	Function Assay	15 μM	1 h	suppresses the activation of and JNK	23441730
U2OS	Function Assay	15 μM	1 h	prevents the LPS- or IL-1-stimulated formation of K63-pUb chains?	23441730
MT‐1?	Function Assay	8?μm	3 h	decreases the levels of p‐STAT3 and p‐4EBP1	23278479
MT‐2?	Function Assay	8?μm	3 h	decreases the levels of p‐STAT3 and p‐4EBP1	23278479
MT‐1?	Function Assay	8?μm	3 h	decreases the levels of the p65 subunit of NF‐κB?	23278479
MT‐2?	Function Assay	8?μm	3 h	decreases the levels of the p65 subunit of NF‐κB?	23278479
MCF-7?	Function Assay	2.5-15 μM	0.5 h	causes the gradual loss of cell adhesion	23093227
HaCaT?	Function Assay	5.0?μM	1?h?	attenuates the TCOH-induced production of IL-6?	23041168
OA chondrocytes?	Function Assay	10 μM	1 h	blocks the AGE-BSA-induced gene/protein expression of GRP78 or COX-2 (p<0.05)	22982228
RAW264.7	Function Assay	15 μM	15-120 min	blocks the production of NO, PGE2, and TNF-α	22745523
RAW264.7	Growth Inhibition Assay	5-30 μM	24 h	inhibits cell growth in a dose-dependent manner	22745523
HBL6	Apoptosis Assay	0.5/5/25 μM	6/24 h	decreases cell viability and leeads to apoptosis in a dose-dependent manner?	22074820
HT29?	Function Assay	1-10 μM	10?h	increases HO-1 mRNA and protein expression	21620964
Ca9–22	Apoptosis Assay	10?μM?	1 h	completely inhibits ALA-PDT-induced apoptosis	21138480
Ca9–22	Function Assay	10?μM?	1 h	completely abrogates the ALA-PDT-induced JNK activation	21138480
A-549	Growth Inhibition Assay	10?μM?	24/48 h	inhibits cell growth in a time-dependent manner	20866043
AP	Function Assay	5/10 μM	48 h	downregulates the BAD protein level a dose-dependent manner	20596645
AQ1	Function Assay	5/10 μM	48 h	downregulates the BAD protein level a dose-dependent manner	20596645
AP	Function Assay	20 μM	4/8 h	downregulates the BAD protein level a time-dependent manner	20596645
AQ1	Function Assay	20 μM	4/8 h	downregulates the BAD protein level a time-dependent manner	20596645
THP-1	Function Assay	5?μM?	0.5 h	attenuates the LPS-induced p-IκBα protein by 72%	20309718
K562	Growth Inhibition Assay	2-30 μM	24 h	IC50=8 μM,inhibits cell growth in a dose-dependent manner	19646807
Jurket	Growth Inhibition Assay	2-30 μM	24 h	IC50=7.1 μM, inhibits cell growth in a dose-dependent manner	19646807
U937	Growth Inhibition Assay	2-30 μM	24 h	IC50=10.5 μM, inhibits cell growth in a dose-dependent manner	19646807
PBMC	Growth Inhibition Assay	2-30 μM	24 h	IC50=40.2 μM, inhibits cell growth in a dose-dependent manner	19646807
K562	Apoptosis Assay	2-20?μM?	24 h	induces a dose-dependent apoptosis	19646807
HEK293	Function assay	20 uM	24 hrs	Inhibition of TNF-alpha stimulated NFkappaB transactivation in HEK293 cells at 20 uM measured after 24 hrs by dual luciferase reporter gene assay	27736063
RAW264.7	Function assay	20 uM	1 hr	Inhibition of LPS-induced NFkB activation in mouse RAW264.7 cells assessed as reduction in nuclear translocation of p65 at 20 uM preincubated for 1 hr followed by LPS stimulation measured after 3 hrs by Western blot method	28667873
RAW264.7	Function assay	20 uM	6 hrs	Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells at 20 uM treated 30 mins before LPS challenge measured after 6 hrs by luciferase reporter gene assay	24315191
RAW264.7	Antinflammatory assay	20 uM	18 hrs	Antinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 20 uM treated 30 mins before LPS challenge measured after 18 hrs by Griess assay	24315191
THP1	Antinflammatory assay	5 uM	24 hrs	Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced extracellular IL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA	24400858
THP1	Antinflammatory assay	5 uM	24 hrs	Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced extracellular TNF-alpha production at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA	24400858
THP1	Antinflammatory assay	5 uM	24 hrs	Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced intracellular proIL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA	24400858
THP1	Antinflammatory assay	5 uM	24 hrs	Antiinflammatory activity in human THP1 cells assessed as inhibition of TPA/ionomycin-induced intracellular IL-1beta level at 5 uM incubated 1 hr prior to TPA/ionomycin challenge measured after 24 hrs by ELISA	24400858
RAW264.7	Function assay	0.3 ug/ml	12 hrs	Inhibition of LPS-induced NF-kB p65 phosphorylation in mouse RAW264.7 cells at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method	28284806
RAW264.7	Function assay	0.3 ug/ml	12 hrs	Inhibition of LPS-induced NF-kB p65 activation in mouse RAW264.7 cells at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by DAPI staining based inverted fluorescence microscopic method	28284806
RAW264.7	Function assay	0.3 ug/ml	12 hrs	Inhibition of NF-kB p65 in mouse RAW264.7 cells assessed as reduction in LPS-induced iNOS expression at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method	28284806
RAW264.7	Function assay	0.3 ug/ml	12 hrs	Inhibition of NF-kB p65 in mouse RAW264.7 cells assessed as reduction in LPS-induced COX2 expression at 0.3 ug/ml preincubated for 12 hrs followed by LPS stimulation for 3 hrs by Western blot method	28284806
HEK293	Function assay	20 uM	24 hrs	Inhibition of TNFalpha-induced NFkappaB activation in HEK293 cells at 20 uM after 24 hrs by dual luciferase reporter gene assay	28873303
RAW264.7	Function assay	20 uM	2 hrs	Inhibition of NFkappaB nuclear translocation in LPS-stimulated mouse RAW264.7 cells at 20 uM pretreated for 2 hrs followed by LPS-induction by DAPI-staining based immunofluorescence microscopic method	29759725
BGC823	Function assay	5 uM	12 hrs	Inhibition of colony formation in human BGC823 cells at 5 uM treated for 12 hrs followed by incubation in drug free medium for 14 days by crystal violet staining based assay	28881286
SGC7901	Function assay	5 uM	12 hrs	Inhibition of colony formation in human SGC7901 cells at 5 uM treated for 12 hrs followed by incubation in drug free medium for 14 days by crystal violet staining based assay	28881286
RAW264.7	Function assay	10 uM	2 hrs	Inhibition of LPS-induced IL-6 mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method	27038497
RAW264.7	Function assay	10 uM	2 hrs	Inhibition of LPS-induced IL-1beta mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method	27038497
RAW264.7	Function assay	10 uM	2 hrs	Inhibition of LPS-induced iNOS mRNA expression in mouse RAW264.7 cells at 10 uM pre-incubated for 2 hrs before LPS stimulation for 24 hrs by qRT-PCR method	27038497
FaDu	Function Assay		2 h	inhibits p65 expression and blocks TNFα-induced TWIST expression	24220622
A549?	Function Assay		1 h	inhibits LTA-induced SP-A mRNA production?significantly	23031213
THP1	Cytotoxicity assay		72 hrs	Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 72 hrs by MTT assay, TC50 = 1.5 μM.	28410442
RAW264.7	Function assay		6 hrs	Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells treated 30 mins before LPS challenge measured after 6 hrs by luciferase reporter gene assay, IC50 = 1.72 μM.	24315191
HEK293	Function assay		6 hrs	Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM.	24533857
HEK293	Function assay		6 hrs	Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM.	24992702
HEK293	Function assay		6 hrs	Inhibition of TNFalpha-induced NF-kappaB activity (unknown origin) transfected in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM.	26343828
HEK293	Function assay		6 hrs	Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 2 μM.	22850207
HEK293	Function assay		6 hrs	Inhibition of TNFalpha-induced human NFkappaB activity in HEK293 cells incubated for 6 hrs followed by compound wash out measured after 5 mins by by luciferase assay, IC50 = 2.01 μM.	22712432
HEK293	Function assay		6 hrs	Inhibition of TNFalpha-induced NFkappaB (unknown origin) activation expressed in HEK293 cells after 6 hrs by luciferase reporter gene assay, IC50 = 5 μM.	23316950
HEK293	Cytotoxicity assay			Cytotoxicity against HEK293 cells, IC50 = 3.8 μM.	24533857
HEK293	Function assay			Effect on Cdc2 expressed in HEK293 cells assessed as effect on Cdc2:Cdc25C interaction complexes in presence of camptothecin by EYFP and/or YFP Venus fragment based reporter gene assay	16680159
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生物活性

產(chǎn)品描述

靶點(diǎn)

E2-conjugating enzymes ^[6] (Cell-free assay)	USP7 ^[7] (Cell-free assay)	USP21 ^[7] (Cell-free assay)	USP6 ^[7] (Cell-free assay)	IκBα?phosphorylation ^[1] (Tumor cells)
	0.19 μM	0.96 μM	1.7 μM	10 μM

體外研究(In Vitro)
體外研究活性	BAY 11-7082完全且特異性地廢除 NF-κB DNA結(jié)合, 下調(diào)NF-κB-誘導(dǎo)的細(xì)胞因子IL-6，且誘導(dǎo)細(xì)胞凋亡。^[1] BAY 11-7082 (< 8 μM) 有效抑制原有的和TNFα 刺激的NF-κB熒光素酶活性，這種作用存在劑量依賴性。BAY 11-7082 (8 μM) 強(qiáng)抑制NCI-H1703 細(xì)胞增殖。 ^[2] Bay 11-7082 (5 μM)作用于感染HTLV-I的T細(xì)胞系，快速且有效的降低NF-κB的DNA結(jié)合力，且下調(diào)抗凋亡基因Bcl-x(L)的表達(dá),而對(duì)另一種轉(zhuǎn)錄因子AP-1與DNA結(jié)合沒有作用效果。Bay 11-7082誘導(dǎo)原代ATL細(xì)胞發(fā)生凋亡比正常的外周血單核細(xì)胞更明顯，而誘導(dǎo)的這些細(xì)胞凋亡也與NF-κB活性的下調(diào)相關(guān)。Bay 11-7082 (5 μM) 選擇性誘導(dǎo)感染HTLV-I的T細(xì)胞系發(fā)生細(xì)胞凋亡，且下調(diào) cyclin D1, cyclin D2, 和 Bcl-xL的表達(dá)。 ^[3] BAY 11-7082 (100 μM)作用于小鼠海馬腦片區(qū)，抑制NMDA引起的p65發(fā)生核易位，也抑制NMDA誘導(dǎo)的NF-κB結(jié)合力的增強(qiáng)。BAY 11-7082抑制NMDA毒性發(fā)生在海馬腦片區(qū)的CA1區(qū)，20 μM時(shí)，對(duì)40％神經(jīng)有保護(hù)作用，100 μM時(shí)，對(duì)70％神經(jīng)有保護(hù)作用。^[4] 作用于脂肪組織，實(shí)驗(yàn)中所有濃度的BAY 11-7082都顯著抑制 NF-κB p65 DNA結(jié)合活性，而作用于骨骼肌，只有50 μM 和 100 μM 的BAY 11-7082顯著抑制NF-κB p65 DNA結(jié)合活性。BAY 11-7082 (100 μM) 作用于人體脂肪組織和骨骼肌，降低IKK-β蛋白。BAY 11-7082 (100 μM) 顯著降低TNF-α從動(dòng)物脂肪組織中釋放，而 IL-6 和 IL-8 的釋放顯著抑制實(shí)驗(yàn)中BAY 11-7082的所有濃度。 BAY 11-7082 (50 μM)作用于骨骼肌，顯著降低 TNF-α, IL-6, 和IL-8 的釋放。^[5] 此外，BAY 11-7082還被發(fā)現(xiàn)抑制了 E2-conjugating酶和E3 ligase酶的活性，從而誘導(dǎo)了B-淋巴癌細(xì)胞和T淋巴癌細(xì)胞的死亡。 ^[6]
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	NCI-H1703 細(xì)胞
	濃度	~8 μM
	孵育時(shí)間	12 小時(shí)
	方法	細(xì)胞在96孔板中轉(zhuǎn)染siRNA，然后在完全NSCLC 培養(yǎng)基中培養(yǎng)72小時(shí)，再使用BAY 11-7082 處理12小時(shí)。細(xì)胞與[³H]胸甘溫育3小時(shí)。使用自動(dòng)細(xì)胞收集器將細(xì)胞收集到過濾器上，然后通過β-閃爍計(jì)數(shù)法測(cè)量放射性。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	NF-κB p-IKKβ/ IκBα p-IRAK4 / IRAK4 NF-κB p-IKKβ/ IκBα p-IRAK4 / IRAK4		31332209
	Growth inhibition assay	Cell viability Cell viability		31332209

參考文獻(xiàn)
[1] Melisi D, et al. Expert Opin Ther Targets, 2007, 11(2), 133-144. [2] Gastonguay A, et al. Cancer Biol Ther, 2012, 13(8), 647-656. [3] Miwatashi S, et al. J Med Chem, 2005, 48(19), 5966-5979. [4] Mori N, et al. Blood, 2002, 100(5), 1828-1834. [5] Goffi F, et al. Neurosci Lett, 2005, 377(3), 147-151. [6] Strickson S, et al. Biochem J. 2013, 451(3), 427-437. [7] Maria Stella Ritorto, et al. Nat Commun . 2014 Aug 27;5:4763. [8] Chen L, et al. J Gastroenterol. 2014 May;49(5):864-74. + 展開

參考文獻(xiàn)

[1] Melisi D, et al. Expert Opin Ther Targets, 2007, 11(2), 133-144.
[2] Gastonguay A, et al. Cancer Biol Ther, 2012, 13(8), 647-656.
[3] Miwatashi S, et al. J Med Chem, 2005, 48(19), 5966-5979.

[4] Mori N, et al. Blood, 2002, 100(5), 1828-1834.
[5] Goffi F, et al. Neurosci Lett, 2005, 377(3), 147-151.
[6] Strickson S, et al. Biochem J. 2013, 451(3), 427-437.
[7] Maria Stella Ritorto, et al. Nat Commun . 2014 Aug 27;5:4763.
[8] Chen L, et al. J Gastroenterol. 2014 May;49(5):864-74.

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化學(xué)信息&溶解度

分子量	207.25	分子式	C₁₀H₉NO₂S
CAS號(hào)	19542-67-7	SDF	Download BAY 11-7082 SDF
Smiles	CC1=CC=C(C=C1)S(=O)(=O)C=CC#N
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 41 mg/mL ( (197.82 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 10 mg/mL (48.25 mM)

Water : Insoluble

DMSO : 41 mg/mL ( (197.82 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 10 mg/mL (48.25 mM)

Water : Insoluble

DMSO : 41 mg/mL ( (197.82 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 3 mg/mL (14.47 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度批次：現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑					動(dòng)物體內(nèi)配方計(jì)算器
	澄清溶液	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	4.0mg/ml (19.30mM)	以 1 mL 工作液為例，取100μL40mg/ml的澄清DMSO儲(chǔ)備液加到400μL PEG300中，混合均勻使其澄清；向上述體系中加入50μLTween80，混合均勻使其澄清；然后繼續(xù)加入450μL ddH2O定容至 1 mL。工作液請(qǐng)現(xiàn)配現(xiàn)用！	動(dòng)物體內(nèi)配方計(jì)算器
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.0mg/ml (9.65mM)	以 1 mL 工作液為例,取50μL40mg/ml的澄清DMSO儲(chǔ)備液加到400μLPEG300中,混合均勻使其澄清;向上述體系中加入50μLTween80,混合均勻使其澄清;然后繼續(xù)加入500μLddH2O定容至1mL。工作液請(qǐng)現(xiàn)配現(xiàn)用!
澄清溶液	5%DMSO 1 Corn oil	8.0mg/ml (38.60mM)	以 1 mL 工作液為例，取50μL160mg/ml的澄清DMSO儲(chǔ)備液加到950μL玉米油中，混合均勻。工作液請(qǐng)現(xiàn)配現(xiàn)用！

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)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(qǐng)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(jìn)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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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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BAY 11-7082

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化學(xué)信息&溶解度

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