| Name | Emivirine |
| Description | Emivirine (MKC-442) is a potent and selective nonnucleoside reverse transcriptase inhibitor for human immunodeficiency virus type 1. |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (3.31 mM), Sonication is recommended. DMSO : 4.8 mg/mL (15.87 mM), Sonication is recommended.
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| Keywords | HIVProtease | HIV-1 | HIV Protease | Emivirine |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Emtricitabine | Dolutegravir intermediate-1 | Dimethyl fumarate | Lamivudine | Chloroquine phosphate | Valproic Acid | (-)-Epigallocatechin Gallate | Decanedioic acid | Dextran sulfate sodium salt (MW 5000) | Tenofovir |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | Anti-Viral Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Infection Compound Library | Human Metabolite Library |