PF-06424439 methanesulfonate

产品编号 T12425Cas号 1469284-79-4

别名

PF-06424439 methanesulfonate 是一种口服有效咪唑并吡啶二酰基甘油酰基转移酶 2 (DGAT2)选择性抑制剂，IC50是14 nM。PF-06424439 methanesulfonate 具有缓慢可逆，时间依赖性的特点，其相对于酰基-CoA 底物以非竞争性模式抑制 DGAT2。

PF-06424439 methanesulfonate

产品编号 T12425Cas号 1469284-79-4

规格	价格	库存
1 mg	¥ 397	现货
5 mg	¥ 788	现货
10 mg	¥ 997	现货
25 mg	¥ 1,980	现货
50 mg	¥ 3,320	现货
100 mg	¥ 4,880	现货
1 mL x 10 mM (in DMSO)	¥ 928	现货

大包装 & 定制

加入购物车

实验操作小课堂

"PF-06424439 methanesulfonate"的相关化合物库

选择批次:

纯度:99.77%

联系我们获取更多批次信息

资源下载

COA HNMR HPLC LCMS LCMS 产品操作手册

TargetMol 的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

产品介绍

生物活性

产品描述	PF-06424439 methanesulfonate, an orally administered, potent, and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM, demonstrates slow reversibility and time-dependent inhibition. It operates in a noncompetitive manner relative to the acyl-CoA substrate, marking its efficacy in targeting DGAT2.
靶点活性	DGAT-2:14 nM
体内活性	PF-06424439 methanesulfonate shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life[1].
动物实验	PF-06424439 methanesulfonate (i.v.; 1 mg/kg) shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life[1].PF-06424439 methanesulfonate (p.o.; 60 mg/kg/day; for 3 days) reduces plasma TG and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-)[1].

化学信息

分子量	536.05
分子式	C₂₃H₃₀ClN₇O₄S
CAS No.	1469284-79-4

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 249 mg/mL (464.50 mM), Sonication is recommended.

H2O: 99 mg/mL (184.68 mM)

溶液配制表

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8655 mL	9.3275 mL	18.6550 mL	93.2749 mL
5 mM	0.3731 mL	1.8655 mL	3.7310 mL	18.6550 mL
10 mM	0.1865 mL	0.9327 mL	1.8655 mL	9.3275 mL
20 mM	0.0933 mL	0.4664 mL	0.9327 mL	4.6637 mL
50 mM	0.0373 mL	0.1865 mL	0.3731 mL	1.8655 mL
100 mM	0.0187 mL	0.0933 mL	0.1865 mL	0.9327 mL