Azamulin

Modify Date: 2024-01-04 14:52:41

Azamulin Structure
Azamulin structure
Common Name Azamulin
CAS Number 76530-44-4 Molecular Weight 478.64800
Density 1.27g/cm3 Boiling Point 659.4ºC at 760 mmHg
Molecular Formula C24H38N4O4S Melting Point 128-130ºC
MSDS Chinese USA Flash Point 352.6ºC
Symbol GHS07
GHS07
Signal Word Warning

 Use of Azamulin


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].

 Names

Name Azamulin
Synonym More Synonyms

 Azamulin Biological Activity

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
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.  

 Chemical & Physical Properties

Density 1.27g/cm3
Boiling Point 659.4ºC at 760 mmHg
Melting Point 128-130ºC
Molecular Formula C24H38N4O4S
Molecular Weight 478.64800
Flash Point 352.6ºC
Exact Mass 478.26100
PSA 156.49000
LogP 4.19070
Index of Refraction 1.59

 Safety Information

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

 Articles1

More Articles
Chemical inhibitors of CYP450 enzymes in liver microsomes: combining selectivity and unbound fractions to guide selection of appropriate concentration in phenotyping assays.

Xenobiotica 45(2) , 95-106, (2014)

1. Chemical inhibition is the widely used method in reaction phenotyping assays for estimation of specific enzyme contribution to a given metabolic pathway. The results from phenotyping assays depend ...

 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