TMC 125 Inhibitor CAS No. 269055-15-4

Cat. No.	Name	Size	Price
KI1181	TMC 125	10 mg	$426
	TMC 125	50 mg	$704
	TMC 125	1 g	$2132

Chemical Characteristic

Product Name	TMC 125
Synonyms	Etravirine, Intelence, R165335
CAS No.	269055-15-4
Molecular Weight	435.28
Formula	C₂₀H₁₅BrN₆O
Chemical Name	4-[6-amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yl]oxy-3,5-dimethylbenzonitrile
Smiles	C(#N)c1cc(c(c(c1)C)Oc1nc(nc(c1Br)N)Nc1ccc(cc1)C#N)C
Chemical Structure

Biological activities

TMC 125 is a nonnucleoside reverse transcriptase (NNRT) inhibitor. TMC 125 is identified as a next-generation NNRT inhibitor. TMC 125 significantly decreases the HIV viral load.^[1] TMC 125 has high activity against wild-type and NNRTI-resistant HIV-1. TMC 125 markedly decreases HIV-1-RNA levels. ^[2] The IC50 of TMC 125 is 38 nM against reverse transcriptase. The EC50 of TMC 125 is ranging from 1.4 to 4.8 nM against HIV-1. In contrast, TMC 125 inhibits HIV-2 with an EC50 of 3.5 µM.^[3] TMC 125 alone significantly decreases exposures of dolutegravir by ca. 70% for AUC_{0-T and by ca. 90% for C_{T.^[4] TMC 125 significantly increases S-warfarin systemic clearance.^[5] TMC 125 is mainly catalyzed by CYPs 3A4, 2C9, and 2C19.^[6]}}

Protocols

In vitro. TMC 125 is dissolved in DMSO.^[6]

References

[1] Etravirine: R165335, TMC 125, TMC-125, TMC125. Drugs R D. 2006, 7(6): 367-373. [2] Mills AM, et al. Efficacy and safety of etravirine (TMC125) in patients with highly resistant HIV-1: primary 24-week analysis. AIDS. 2007, 21(6): F1-F10. [3] Andries K, et al. TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2004, 48(12): 4680-4686. [4] Song I, et al. Effects of etravirine alone and with ritonavir-boosted protease inhibitors on the pharmacokinetics of dolutegravir. Antimicrob Agents Chemother. 2011, 55(7): 3517-3521. [5] John J, et al. Effects of Etravirine on the Pharmacokinetics and Pharmacodynamics of Warfarin in Rats. Br J Pharmacol. 2012 [6] Yanakakis LJ, et al. Biotransformation of the antiretroviral drug etravirine: metabolite identification, reaction phenotyping, and characterization of autoinduction of cytochrome P450-dependent metabolism. Drug Metab Dispos. 2012, 40(4): 803-814.

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