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AMG 837 calcium hydrate 是口服有效的 GPR40/FFA1部分激动剂,抑制 [3H]AMG 837 与人类 FFA1受体的特异性结合,pIC50为 8.13。AMG 837 calcium hydrate 可增强啮齿动物的胰岛素分泌并降低葡萄糖水平。
AMG 837 calcium hydrate 是口服有效的 GPR40/FFA1部分激动剂,抑制 [3H]AMG 837 与人类 FFA1受体的特异性结合,pIC50为 8.13。AMG 837 calcium hydrate 可增强啮齿动物的胰岛素分泌并降低葡萄糖水平。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 188 | 现货 | |
5 mg | ¥ 447 | 现货 | |
10 mg | ¥ 678 | 现货 | |
25 mg | ¥ 1,600 | 现货 | |
50 mg | ¥ 2,350 | 现货 | |
100 mg | ¥ 3,400 | 现货 | |
200 mg | ¥ 4,770 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 498 | 现货 |
产品描述 | AMG 837 calcium hydrate is a potent GPR40 agonist with an EC50 of 13 nM. AMG 837 calcium hydrate also shows highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM). |
靶点活性 | FFA1/GPR40:13 nM (EC50) |
体外活性 | GPR40 agonist AMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50: 13 nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50s: 23/13 nM). AMG 837 was a partial agonist on GPR40 with maximal activity 85% of that shown by DHA. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50: 3 μM) on the α2-adrenergic receptor [1]. |
体内活性 | In rats, AMG 837 increases insulin release when glucose levels are elevated [2]. |
分子量 | 950.97 |
分子式 | C52H44CaF6O8 |
CAS No. | 1259389-38-2 |
Smiles | [H]O[H].[H]O[H].O=C([O-])C[C@H](C#CC)C1=CC=C(OCC2=CC(C3=CC=C(C(F)(F)F)C=C3)=CC=C2)C=C1.O=C([O-])C[C@H](C#CC)C4=CC=C(OCC5=CC(C6=CC=C(C(F)(F)F)C=C6)=CC=C5)C=C4.[Ca+2] |
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: 40 mg/mL (87.83 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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