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Emivirine

Catalog No. T27260 CAS 149950-60-7

Synonyms: MKC442, MKC-442, MKC 442, DRG-0302, DRG 0302, DRG0302

Emivirine (MKC-442) is a potent and selective nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1.

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Emivirine, CAS 149950-60-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 50.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 346.00
50 mg	In stock	$ 516.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Purity: 99.68%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Emivirine (MKC-442) is a potent and selective nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1.
Targets&IC50	RNA polymerase activity (dGTP-dependent):0.01μM(ki), DNA polymerase activity (dTTP-dependent):0.20μM(ki)
In vitro	Emivirine is a novel nonnucleoside reverse transcriptase inhibitor that displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity in vivo. IC50 against laboratory-adapted strains of HIV-1 ranged from 1.6 to 19 nM. Against clinical isolates, the IC50 for EMV ranged from 2 to 40 nM. The Ki values of 0.20 and 0.01 μM for dTTP- and dGTP-dependent DNA or RNA polymerase activity, respectively[1].
In vivo	Emivirine displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity in vivo. Pharmacokinetics were linear for both rats and monkeys, and oral absorption was 68% in rats. Rats were given an oral dose of Emivirine at 10 mg/kg of body weight showed widespread distribution in tissue after 30 min. In rats given an oral dose of 250 mg/kg, there were equal levels of Emivirine in the plasma and the brain[2].

Synonyms	MKC442, MKC-442, MKC 442, DRG-0302, DRG 0302, DRG0302
Molecular Weight	302.37
Formula	C17H22N2O3
CAS No.	149950-60-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.8 mg/mL (15.87 mM)

References and Literature

1. Panita Decha, et al. Theoretical studies on the molecular basis of HIV-1RT/NNRTIs interactions. J Enzyme Inhib Med Chem. 2011 Feb;26(1):29-36. 2. Szczech GM, et al. Safety assessment, in vitro and in vivo, and pharmacokinetics of emivirine, a potent and selective nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2000 Jan;44(1):123-30. 3. Boudet N, Knochel P. Chemo- and regioselective functionalization of uracil derivatives. Applications to the synthesis of oxypurinol and emivirine. Org Lett. 2006 Aug 17;8(17):3737-40. PubMed PMID: 16898805. 4. Petersen L, Jørgensen PT, Nielsen C, Hansen TH, Nielsen J, Pedersen EB. Synthesis and evaluation of double-prodrugs against HIV. Conjugation of D4T with 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine)-type reverse transcriptase inhibitors via the SATE prodrug approach. J Med Chem. 2005 Feb 24;48(4):1211-20. PubMed PMID: 15715487.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Clinical Compound Library Bioactive Compounds Library Max Anti-Viral Compound Library Bioactive Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Emivirine 149950-60-7 Microbiology/Virology Proteases/Proteasome HIV Protease MKC442 MKC-442 MKC 442 DRG-0302 DRG 0302 DRG0302 inhibitor inhibit

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