Ibipinabant | CB1 antagonist | Probechem Biochemicals

Chemical Structure : Ibipinabant

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Ibipinabant (SLV-319, BMS-646256)

货号: PC-20522Not For Human Use, Lab Use Only.

Ibipinabant (SLV319, BMS-646256) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor with Ki of 7.8 nM, >1000-fold selectivity for CB1 over CB2.

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生物&药学活性

Ibipinabant (SLV319, BMS-646256) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor with Ki of 7.8 nM, >1000-fold selectivity for CB1 over CB2.
SLV319 concentration dependently antagonizes WIN-55212 (CB1 agonist)-induced arachidonic acid release in CHO cells with pA2 of 9.9.
SLV319 (3 mg/kg/day; p.o. for 28 d) reduces the food intake, body weight, and hormonal/metabolic abnormalities in diet-induced obesity (DIO) mice.
SLV319 (3 mg/kg/day, p.o. for 28 d) reverses the HFD-induced increase in adipose tissue leptin mRNA.
SLV319 (3-10 mg/kg; daily oral gavage) has weight loss-independent antidiabetic effects and attenuates β-cell loss in a rat model of progressive β-cell dysfunction.

物理化学性质&存储条件

分子量	487.40
分子式	C23H20Cl2N4O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	C/N=C(N1N=C(C2=CC=C(Cl)C=C2)[C@@H](C3=CC=CC=C3)C1)/NS(=O)(C4=CC=C(Cl)C=C4)=O

参考文献

1. Lange JHM, et, al. J Med Chem. 2004 Jan 29;47(3):627-43.

2. Tam J, et, al. Cell Metab. 2012 Aug 8;16(2):167-79.

3. Rohrbach K, et, al. Diabetes Obes Metab. 2012 Jun;14(6):555-64.

Ibipinabant (SLV-319, BMS-646256)

生物&药学活性

物理化学性质&存储条件

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Ibipinabant (SLV-319, BMS-646256)

生物&药学活性

物理化学性质&存储条件

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