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Emivirine

Cat. No. M28542
Emivirine Structure
Synonym:

MKC-442

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Biological Activity

Emivirine (MKC-442) is a non-nucleoside reverse transcriptase inhibitors (NNRTIs) with Ki values of 0.20 and 0.01 μM for dTTP- and dGTP-dependent DNA or RNA polymerase activity, respectively. Emivirine displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity.

Chemical Information
Molecular Weight 302.37
Formula C17H22N2O3
CAS Number 149950-60-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Willem D F Venter, et al. N Engl J Med. Dolutegravir plus Two Different Prodrugs of Tenofovir to Treat HIV

[2] N R El-Brollosy, et al. Drug Res (Stuttg). Synthesis and Antiviral Evaluation of 1-[(2-Phenoxyethyl)oxymethyl] and 6-(3,5-Dimethoxybenzyl) Analogues of HIV Drugs Emivirine and TNK-651

[3] Nadège Boudet, et al. Org Lett. Chemo- and regioselective functionalization of uracil derivatives. Applications to the synthesis of oxypurinol and emivirine

[4] N Cheonis. BETA. Emivirine: an NRTI that functions as an NNRTI

[5] A L Hopkins, et al. J Med Chem. Design of MKC-442 (emivirine) analogues with improved activity against drug-resistant HIV mutants

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Keywords: Emivirine, MKC-442 supplier, HIV Protease, inhibitors, activators


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