Azamulin
- Product Name
- Azamulin
- CAS No.
- 76530-44-4
- Chemical Name
- Azamulin
- Synonyms
- Azamulin; SA 85530b;TMD 85-530, SA 85530b;Antibiotic TDM 85-530;14-O-(5-(2-Amino1,3,4-triazolyl)thioacetyl)dihydromutilin;[(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;Acetic acid, 2-[(3-amino-1H-1,2,4-triazol-5-yl)thio]-, (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
- CBNumber
- CB51176138
- Molecular Formula
- C24H38N4O4S
- Formula Weight
- 478.65
- MOL File
- 76530-44-4.mol
Azamulin Property
- 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)
- form
- powder
- pka
- 9.56±0.40(Predicted)
- color
- white to beige
- Stability:
- Store at -2℃.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML0485
- Product name
- Azamulin
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $201
- Updated
- 2024/03/01
- Product number
- SML0485
- Product name
- Azamulin
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $774
- Updated
- 2024/03/01
- Product number
- 18748
- Product name
- Azamulin
- Purity
- ≥98%
- Packaging
- 500μg
- Price
- $45
- Updated
- 2024/03/01
- Product number
- 18748
- Product name
- Azamulin
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $73
- Updated
- 2024/03/01
- Product number
- 18748
- Product name
- Azamulin
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $180
- Updated
- 2024/03/01
Azamulin Chemical Properties,Usage,Production
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
Uses
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.
Uses
It is a highly selective human CYP3A4 inhibitor. A mutilin derivative
Uses
Azamulin has been used as a selective CYP3A4 inhibitor to pretreat primary hepatocyte cells and in prostate cancer cell lines LNCaP and MDAPCa2b.
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).
Azamulin Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Azamulin manufacturers
- Product
- Azamulin 76530-44-4
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- ≥98%
- Supply Ability
- g/kg/Ton
- Release date
- 2019-12-25