产品说明书

BVT948

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Chemical Structure| 39674-97-0 同义名 : -
CAS号 : 39674-97-0
货号 : A545026
分子式 : C14H11NO3
纯度 : 99%+
分子量 : 241.242
MDL号 : MFCD00616487
存储条件:

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(435.25 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Protein tyrosine phosphatases (PTPs) play a multifunctional role in coordinating signaling networks. BVT 948 is an inhibitor of PTPs with IC50 values of 0.9±0.3μM, 1.7±0.1μM, 0.09±0.01μM, 1.5±0.4μM, and 0.7±0.05μM for PTP1B, TCPTP, SHP-2, LAR, and YopH, respectively. It also exhibited robust inhibitory effects against several cytochrome P450 isoforms in vitro. BVT 948 at a concentration of 25μM stimulated glucose uptake into L6 myotubes in a PI3K-dependent fashion. Mice treated with 3μmol/kg BVT 948 showed significantly increased glucose clearance from the bloodstream in response to insulin compared with the vehicle-treated group.[1]
作用机制 BVT 948 is a noncompetitive inhibitor of PTP. It irreversibly inhibits PTP1B activity in vitro by catalyzing the catalytic cysteine residue of the enzyme.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.15mL

0.83mL

0.41mL

20.73mL

4.15mL

2.07mL

41.45mL

8.29mL

4.15mL

参考文献

[1]Liljebris C, Baranczewski P, Björkstrand E, Byström S, Lundgren B, Tjernberg A, Warolén M, James SR. Oxidation of protein tyrosine phosphatases as a pharmaceutical mechanism of action: a study using 4-hydroxy-3,3-dimethyl-2H-benzo[g]indole-2,5(3H)-dione. J Pharmacol Exp Ther. 2004 May;309(2):711-9. doi: 10.1124/jpet.103.062745