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Raltegravir
- MK-0518
- Soluble in DMSO
- MF: C20H21FN6O5
- MW: 444.42
Description
Raltegravir is a potent, selective and orally bioavailable HIV-integrase inhibitor with an IC50 value of 0.015 μM for inhibition of strand transfer. Also, Raltegravir showed potency in a cell based assay with CIC95 values of 0.019 and 0.031 µM in 10% FBS and 50% NHS, respectively.
More Information
| Parent CAS No. | 518048-05-0 |
|---|---|
| Chemical Name | N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide |
| SMILES | N1(C)C(=O)C(O)=C(C(=O)NCC2C=CC(F)=CC=2)N=C1C(C)(C)NC(=O)C1OC(C)=NN=1 |
| MFCD | MFCD10698872 |
| InChi | InChI=1S/C20H21FN6O5/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30) |
| InChiKey | CZFFBEXEKNGXKS-UHFFFAOYSA-N |
| CID | 54671008 |
| Short Description | HIV integrase inhibitor |
References
- M Markowitz et al. Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals. J Acquir Immune Defic Syndr. 2006 Dec 15;43(5):509-15.
- V Summa et al. Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. J Med Chem. 2008 Sep 25;51(18):5843-55.
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