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Zamicastat (BIA 5-1058) 是多巴胺 β-羟化酶 (DBH) 抑制剂,可透过血脑屏障引起中枢和周边效应,具有降血压作用。它也是一种浓度依赖性的双重 P-gp 和 BCRP 抑制剂,IC50值分别为 73.8 和 17.0 μM。
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Zamicastat (BIA 5-1058) 是多巴胺 β-羟化酶 (DBH) 抑制剂,可透过血脑屏障引起中枢和周边效应,具有降血压作用。它也是一种浓度依赖性的双重 P-gp 和 BCRP 抑制剂,IC50值分别为 73.8 和 17.0 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 762 | 现货 | |
5 mg | ¥ 1,890 | 现货 | |
10 mg | ¥ 2,970 | 现货 | |
25 mg | ¥ 5,530 | 现货 | |
50 mg | ¥ 8,280 | 现货 | |
100 mg | ¥ 10,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,980 | 现货 |
产品描述 | Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH), and is also a concentration-dependent dual inhibitor of P-gp and BCRP(IC50 values of 73.8 μM and 17.0 μM, respectively). |
靶点活性 | P-gp:73.8 μM , Dopamine β-hydroxylase:, BCRP:17.0 μM |
体内活性 | In the Dahl SS rat, Zamicastat (10, 30 and 100 mg/kg/day; oral bolus, 7 days) is tested acutely against salt-induced hypertension. Zamicastat produces a dose-dependent decrease in blood pressure[2]. |
别名 | BIA 5-1058 |
分子量 | 401.47 |
分子式 | C21H21F2N3OS |
CAS No. | 1080028-80-3 |
Smiles | Fc1cc(F)c2OC[C@@H](Cc2c1)n1c(CCNCc2ccccc2)c[nH]c1=S |
密度 | 1.36 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: 150 mg/mL (373.63 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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