Azamulin Struktur

Azamulin

Bezeichnung:Azamulin

CAS-Nr76530-44-4

Englisch Name:Azamulin

CBNumberCB51176138

SummenformelC24H38N4O4S

Molgewicht478.65

MOL-Datei76530-44-4.mol

Azamulin physikalisch-chemischer Eigenschaften

Schmelzpunkt	128-130°C
Siedepunkt	659.4±65.0 °C(Predicted)
Dichte	1.27±0.1 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	DMSO: soluble10mg/mL (clear solution)
Aggregatzustand	powder
pka	9.56±0.40(Predicted)
Farbe	white to beige
Stabilität	Store at -2℃.

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26
WGK Germany	3

Gefahreninformationscode (GHS)

Azamulin Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Chemische Eigenschaften
White Solid
Verwenden
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.
Verwenden
It is a highly selective human CYP3A4 inhibitor. A mutilin derivative
Verwenden
Azamulin has been used as a selective CYP3A4 inhibitor to pretreat primary hepatocyte cells and in prostate cancer cell lines LNCaP and MDAPCa2b.
Allgemeine Beschreibung
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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

76530-44-4, Azamulin Verwandte Suche:

Send Inquriy