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Zamicastat

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。

CAS号

1080028-80-3

分子式

C21H21F2N3OS

主要靶点

BCRP|Hydroxylase|P-gp

仅限科研使用

Cat No : CM11767

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Synonyms

BIA 5-1058

验证数据展示

  • CAS No.: 1080028-80-3

    Zamicastat
    CAS#: 1080028-80-3

产品信息

Zamicastat 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).

CAS号 1080028-80-3
分子式 C21H21F2N3OS
主要靶点 BCRP|Hydroxylase|P-gp
主要通路 代谢|神经科学|离子通道
分子量 401.47
纯度 97.43%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 BIA 5-1058

靶点活性

Dopamine β-hydroxylase:|P-gp:73.8 μM |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].

溶解度

DMSO:150 mg/mL (373.63 mM),Sonification is recommended.

参考文献

1.Bicker J, et al. In vitro assessment of the interactions of dopamine β-hydroxylase inhibitors with human P-glycoprotein and Breast Cancer Resistance Protein. Eur J Pharm Sci. 2018 May 30;117:35-40. 2.Igreja B, et al. Effects of Zamicastat treatment in a genetic model of salt-sensitive hypertension and heart failure. Eur J Pharmacol. 2019 Jan 5;842:125-132.

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