| Bioactivity | Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin is an oral corticosteroid for asthma study[1][2][3]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | Troleandomycin markedly suppresses these microsomal side chain hydroxylations in both mouse and human livers in a dose-dependent manner[2]. Animal Model: | ||||||||||||
| Name | Troleandomycin | ||||||||||||
| CAS | 2751-09-9 | ||||||||||||
| Formula | C41H67NO15 | ||||||||||||
| Molar Mass | 813.97 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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. [3]. D J Evans, et al. Troleandomycin as an oral corticosteroid steroid sparing agent in stable asthma. Cochrane Database Syst Rev. 2001;(2):CD002987. |
Troleandomycin
CAS: 2751-09-9 F: C41H67NO15 W: 813.97
Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin
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