TroleandomycinTroleandomycin
MedChemExpress (MCE)
HY-108881
2751-09-9
Triacetyloleandomycin
98.0%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin is an oral corticosteroid for asthma study.
Troleandomycin markedly inhibits 6β-hydroxylation of testosterone, 25- and 26-hydroxylations of 5β-cholestane-3α,7α,12α-triol and 23R-, 24R-, 24S-, and 27-hydroxylations of 5β-cholestane-3α,7α,12α,25-tetrol in both recombinant CYP3A4 and microsomes, but IC50 values for microsomes are somewhat higher than those for recombinant CYP3A4[1].
Troleandomycin markedly suppresses these microsomal side chain hydroxylations in both mouse and human livers in a dose-dependent manner[2].
CYP3
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[1]. Shingen Misaka, et al. Green tea extract affects the cytochrome P450 3A activity and pharmacokinetics of simvastatin in rats. Drug Metab Pharmacokinet. 2013
28(6):514-8. [Content Brief]
[2]. A Honda, et al. Side chain hydroxylations in bile acid biosynthesis catalyzed by CYP3A are markedly up-regulated in Cyp27-/- mice but not in cerebrotendinous xanthomatosis. J Biol Chem. 2001 Sep 14
276(37):34579-85. [Content Brief]
[3]. D J Evans, et al. Troleandomycin as an oral corticosteroid steroid sparing agent in stable asthma. Cochrane Database Syst Rev. 2001
(2):CD002987. [Content Brief]