76530-44-4

76530-44-4 structure

Name: Azamulin
Chemical Name: Azamulin
CAS Number: 76530-44-4
Molecular Formula: C₂₄H₃₈N₄O₄S
Molecular Weight: 478.64800
Catalog: Signaling Pathways Metabolic Enzyme/Protease Cytochrome P450
Create Date: 2018-02-08 08:00:00
Modify Date: 2024-01-04 14:52:41
Azamulin is an irreversible, highly selective inhibitior of human CYP3Aa. Azamulin has CYP3A inhibition activity with IC50 values range from 0.03-0.24 μM. Azamulin can be used for the research of metabolism and antiinfection[1].

Name	Azamulin
Synonyms	(3aS,4R,5S,6R,8R,9R,9aR,10R)-6-Ethyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propanocyclopentacycloocten-8-yl ((5-amino-1,2,4-triazol-3-yl)thio)acetat ((5-Amino-s-triazol-3-yl)thio)acetic acid,8-ester with (3aS,4R,5S,6R,8R,9aR,10R)-6-ethyloctahydro-5,8-dihydroxy-4,6,9,10-tetramethyl-3a,9-propano-3aH-cyclopentacycloocten-1(4H)-one UNII-875AQ866X1

Description	Azamulin is an irreversible, highly selective inhibitior of human CYP3Aa. Azamulin has CYP3A inhibition activity with IC50 values range from 0.03-0.24 μM. Azamulin can be used for the research of metabolism and antiinfection[1].
Related Catalog	Research Areas >> Infection Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450 Research Areas >> Metabolic Disease
Target	CYP3A:0.03-0.24 μM (IC50)
In Vitro	Azamulin 具有 CYP3A 抑制活性，IC50 值范围为 0.03-0.24 μM[1]。 Azamulin 对 CYP3A 的抑制呈 S 型曲线，并且对底物 7-benzyloxy-4-trifluoromethylcoumarin, testosterone 和 midazolam 表现良好[1]。 Azamulin (4.8 μM; 10 min) 在 NADPH 存在的情况下抑制约 95% 的睾酮 6β-羟化酶活性[1]。 Azamulin 在乙腈中储存长达 12 天时表现出良好的化学稳定性[1]。
References	[1]. David M Stresser, et al. Highly selective inhibition of human CYP3Aa in vitro by azamulin and evidence that inhibition is irreversible. Drug Metab Dispos. 2004 Jan;32(1):105-12.

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H315-H319-H335
Precautionary Statements	P261-P305 + P351 + P338
RIDADR	NONH for all modes of transport