IDX899 - CAS 1097733-15-7
Catalog number: 1097733-15-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H17ClN3O3P
Molecular Weight:
413.79
COA:
Inquire
Targets:
NNRTIs
Description:
IDX899 is a novel next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) with activity against efavirenz-resistant strains. It is used in the treatment of treatment-naive HIV-1-infected subjects.
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Purity:
95%
Appearance:
Solid powder
Synonyms:
IDX-899;5-Chloro-3-[[3-[(E)-2-cyanovinyl]-5-methyl-phenyl]-methoxy-phosphoryl]-1H-indole-2-carboxamide;Methyl (E)-(2-carbamoyl-5-chloro-1H-indol-3-yl)(3-(2-cyanovinyl)-5-methylphenyl)phosphinate;GSK-224876;GSK224876;(R,E)-methyl (2-carbamoyl-5-chloro-1H-indol-3-yl)(3-(2-cyanovinyl)-5-methylphenyl)phosphinate
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
IDX899 is used in the treatment of treatment-naive HIV-1-infected subjects.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
CGBYTKOSZYQOPV-ONEGZZNKSA-N
InChI:
InChI=1S/C20H17ClN3O3P/c1-12-8-13(4-3-7-22)10-15(9-12)28(26,27-2)19-16-11-14(21)5-6-17(16)24-18(19)20(23)25/h3-6,8-11,24H,1-2H3,(H2,23,25)/b4-3+
Canonical SMILES:
CC1=CC(=CC(=C1)C=CC#N)P(=O)(C2=C(NC3=C2C=C(C=C3)Cl)C(=O)N)OC
1.IDX-899, an aryl phosphinate-indole non-nucleoside reverse transcriptase inhibitor for the potential treatment of HIV infection.
Klibanov OM1, Kaczor RL. Curr Opin Investig Drugs. 2010 Feb;11(2):237-45.
Antiretroviral drug resistance is one of the complications of highly active antiretroviral therapy (HAART). Second-generation non-nucleoside reverse transcriptase inhibitors (NNRTIs) are being developed for use in patients infected with HIV-1 because of the enhanced activity of these inhibitors against viruses that are resistant to the first-generation NNRTIs. IDX-899 (GSK-2248761), under development by Idenix Pharmaceuticals Inc and ViiV Healthcare, is an aryl phosphinate-indole second-generation NNRTI that potently and selectively inhibits wild-type and NNRTI-resistant HIV-1 in vitro. Preclinical data for IDX-899 suggest a significantly greater barrier to resistance compared with that of the first-generation NNRTI efavirenz. Two pathways of resistance have been identified for IDX-899 in vitro that include Glu138Lys and Val90Ile/Tyr181Cys mutations. Pharmacokinetic studies demonstrated that IDX-899 exhibits linear, dose-proportional and food-dependent pharmacokinetics; Cmin concentrations achieved with this drug allow once-daily dosing.
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CAS 1097733-15-7 IDX899

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