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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 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
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 |
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]. |
分子量 | 536.05 |
分子式 | C23H30ClN7O4S |
CAS No. | 1469284-79-4 |
Smiles | CS(O)(=O)=O.Clc1cnn(c1)C1(CC1)c1nc2ccc(nc2[nH]1)N1CCC[C@H](C1)C(=O)N1CCCC1 |
密度 | no data available |
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 | ||||||||||||||||||||||||||||||||||||
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