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AMG-1694 是一种强效的葡萄糖激酶-葡萄糖激酶调节蛋白(GK-GKRP)干扰物,能促进 GK-GKRP 复合物的解离,其 IC50 值为 7 nM,从而间接提高 GK 酶的活性。AMG-1694 可使几种啮齿动物糖尿病模型的血糖水平恢复正常,并降低糖尿病动物而非正常血糖动物的血糖。AMG-1694 能有效逆转 GKRP 对 GK 活性的抑制作用,并促进 GK 转位。
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AMG-1694 是一种强效的葡萄糖激酶-葡萄糖激酶调节蛋白(GK-GKRP)干扰物,能促进 GK-GKRP 复合物的解离,其 IC50 值为 7 nM,从而间接提高 GK 酶的活性。AMG-1694 可使几种啮齿动物糖尿病模型的血糖水平恢复正常,并降低糖尿病动物而非正常血糖动物的血糖。AMG-1694 能有效逆转 GKRP 对 GK 活性的抑制作用,并促进 GK 转位。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 2,670 | 现货 | |
5 mg | ¥ 6,360 | 现货 | |
10 mg | ¥ 8,690 | 现货 | |
25 mg | ¥ 12,900 | 现货 | |
50 mg | ¥ 15,300 | 现货 | |
100 mg | ¥ 19,500 | 现货 | |
500 mg | ¥ 38,800 | 现货 |
产品描述 | AMG-1694, a potent disruptor of the glucokinase–glucokinase regulatory protein (GK-GKRP) complex, operates by promoting the dissociation of this complex, thereby indirectly enhancing GK enzymatic activity with an IC50 of 7 nM. It effectively normalizes blood glucose levels in various rodent diabetes models [1] and lowers blood glucose specifically in diabetic animals without affecting normoglycemic ones. Additionally, AMG-1694 reverses the GKRP-induced inhibition of GK activity and facilitates GK translocation. |
靶点活性 | GK:0.02 μM(EC50), GK-GKRP:7 nM |
体外活性 | AMG-1694在GKRP存在下,高效地恢复了GK的酶活性,其EC50为0.020 μM。[1] |
分子量 | 533.63 |
分子式 | C23H30F3N3O4S2 |
CAS No. | 1361217-07-3 |
Smiles | C([C@@H]1N(CCN(S(=O)(=O)C2=CC=CS2)C1)C3=CC=C([C@@](C(F)(F)F)(C)O)C=C3)N4[C@@H](C)COCC4 |
密度 | 1.348 g/cm3 (Predicted) |
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: 50 mg/mL (93.7 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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