Azamulin

A selective CYP3A inhibitor

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库存: 现货

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促销价

数量
500ug

￥800.00

640.00

- +
1mg

￥1525.00

1220.00

- +
5mg

￥2587.00

2070.00

- +

已选 0 种 0 瓶

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货号: ajci70018
CAS: 76530-44-4
别名: 阿扎莫林,Antibiotic TDM 85-530
分子式: C24H38N4O4S
分子量: 478.7
纯度: >98%
溶解度: 20mg/mL in ethanol, or in DMSO, or in DMF
储存: Store at -20°C
库存: 现货

Background

Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources). [1] It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms. [1] Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.[2]?

Reference:
[1]. Stresser, D.M., Broudy, M.I., Ho, T., et al. Highly selective inhibition of human CYP3Aa in vitro by azamulin and evidence that inhibition is irreversible. Drug Metabolism and Disposition 32(1), 105-112 (2004).
[2]. Lim, H.K., Duczak, N., Jr., Brougham, K., et al. Automated screening with confirmation of mechanism-based inactivation of CYP3A4, CYP2C9, CYP2C19, CYP2D6, and CYP1A2 in pooled human liver microsomes. Drug Metabolism and Disposition 33(8), 1211-1219 (2005).