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HomeProduct name listAzamulin

Azamulin

Synonym(s):(5-Amino-1H-1,2,4-triazol-3-yl)thio]acetic acid (3aS,4R,5S,6R,8R,9R,9aR,10R)-6-ethyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3aH-cyclopentacycloocten-8-yl ester;;14-O-(5-(2-Amino1,3,4-triazolyl)thioacetyl)dihydromutilin;Antibiotic TDM 85-530

Azamulin Structural

What is Azamulin?

Description

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). It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms. Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.

Chemical properties

White Solid

The Uses of Azamulin

Azamulin is a semi-synthetic pleuromutilin prepared by sequential reaction of dihydropleuromutilin tosylate with 2-amino-1,2,4-triazole-5-thiol. While azamulin is a broad spectrum antibiotic in the pleuromutilin class, this aspect of its bioprofile has received little attention. In fact, the triazole substituent added to nominally improve the drugs bioavailability, imparted an unusual selectivity for the inhibition of specific cytochrome P450 mixed function oxidase sub-types, important for understanding the manner in which the body metabolises drugs or xenobiotics.

The Uses of Azamulin

It is a highly selective human CYP3A4 inhibitor. A mutilin derivative

The Uses of Azamulin

Azamulin has been used as a selective CYP3A4 inhibitor to pretreat primary hepatocyte cells and in prostate cancer cell lines LNCaP and MDAPCa2b.

What are the applications of Application

Azamulin is a highly selective CYP3A4 inhibitor & a mutilin derivative

General Description

Azamulin isolated from fungus Pleurotus mutilis is a diterpene antibiotic. It is related to pleuromutilin being its synthetic azole derivative.

Biochem/physiol Actions

Azamulin is a derivative of the antibiotic pleuromutilin. The compound is a very specific inhibitor of the CYP3A family (IC50 = 0.03-0.24 μM). Azamulin is 15 and 13 fold more active against CYP3A4 compared to CYP3A5 or CYP3A7, respectively, and is at least 100 fold selective over other CYP isoforms, with the exception of CYP2J2 (approximately 50-fold).

Properties of Azamulin

Melting point: 128-130°C
Boiling point: 659.4±65.0 °C(Predicted)
Density  1.27±0.1 g/cm3(Predicted)
storage temp.  -20°C
solubility  DMSO: soluble10mg/mL (clear solution)
pka 9.56±0.40(Predicted)
form  powder
color  white to beige
Stability: Store at -2℃.

Safety information for Azamulin

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P264:Wash hands thoroughly after handling.
P264:Wash skin thouroughly after handling.
P271:Use only outdoors or in a well-ventilated area.
P280:Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352:IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for Azamulin

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