Islatravir
Cat. No.：YN250100
| 产品名称: | Islatravir |
| CAS No.: | 865363-93-5 |
| Chemical Name: | 2′-deoxy-4′-C-ethynyl-2-fluoro-adenosine |
| Synonyms: | MK-8591 |
| 分子量: | 293.25 |
| 分子式: | C₁₂H₁₂FN₅O₃ |
| SMILES: | OC[C@]1(C#C)[C@H](C[C@H](N2C=NC3=C2N=C(F)N=C3N)O1)O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Islatravir (MK-8591) 是一种核苷逆转录酶 (reverse transcriptase) 抑制剂，具有抗HIV-1活性，对 HIV-1 (WT)，HIV-1 (M184V)，HIV-1 (MDR) 的EC50值分别为 0.068 nM，3.1 nM 和 0.15 nM。 |
| IC50和靶点: | [{name:"HIV-1 (WT):0.068 nM (EC50)"},{name: "HIV-1 (MDR):0.15 nM (EC50)"},{name: "HIV-1 (M184V):3.1 nM (EC50)"}] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Michailidis, E., Huber, A.D., Ryan, E.M., et al.4'-Ethynyl-2-fluoro-2'-deoxyadenosine (EFdA) inhibits HIV-1 reverse transcriptase with multiple mechanismsJ. Biol. Chem.289(35),24533-24548(2014)
Markowitz, M., and Sarafianos, S.G.4'-Ethynyl-2-fluoro-2'-deoxyadenosine, MK-8591: A novel HIV-1 reverse transcriptase translocation inhibitorCurr. Opin. HIV AIDS13(4),294-299(2018)
Kawamoto, A., Kodama, E., Sarafianos, S.G., et al.2'-deoxy-4'-C-ethynyl-2-halo-adenosines active against drug-resistant human immunodeficiency virus type 1 variantsInt. J. Biochem. Cell Biol.40(11),2410-2420(2008)
Stoddart, C.A., Galkina, S.A., Joshi, P., et al.Oral administration of the nucleoside EFdA (4'-ethynyl-2-fluoro-2'-deoxyadenosine) provides rapid suppression of HIV viremia in humanized mice and favorable pharmacokinetic properties in mice and the rhesus macaqueAntimicrob. Agents Chemother.59(7),4190-4198(2015)
