Fosdevirine - CAS 1018450-26-4
Catalog number: 1018450-26-4
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H17ClN3O3P
Molecular Weight:
413.80
COA:
Inquire
Targets:
NNRTIs
Description:
Fosdevirine is a highly potent next-generation Anti-HIV nonnucleoside reverse transcriptase inhibitor (NNRTI) with an EC50 of 11 nM. It is a novel and once-daily (QD) inhibitor with activity against efavirenz-resistant strains. It demonstrated potent antiviral activity in treatment-naive HIV-infected subjects, and had favorable PK and resistance profiles. It was originally developed by idenix pharmaceuticals and was in clinical phase 2, but now it has been terminated.
Publictions citing BOC Sciences Products
  • >> More
Purity:
95%
Appearance:
Solid powder
Synonyms:
GSK2248761;GSK-2248761;GSK2248761A;GSK-2248761A;IDX899;IDX-899;Methyl (E)-(2-carbamoyl-5-chloro-1H-indol-3-yl)(3-(2-cyanovinyl)-5-methylphenyl)phosphinate;5-Chloro-3-[[3-[(E)-2-cyanoethenyl]-5-methylphenyl]-methoxyphosphoryl]-1H-indole-2-carboxamide
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Fosdevirine has potent antiviral activity.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Boiling Point:
686.4±65.0 °C | Condition: Press: 760 Torr
Density:
1.42±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
CGBYTKOSZYQOPV-ASSBYYIWSA-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+/t28-/m1/s1
Canonical SMILES:
CC1=CC(=CC(=C1)C=CC#N)P(=O)(C2=C(NC3=C2C=C(C=C3)Cl)C(=O)N)OC
Current Developer:
Fosdevirine was originally developed by idenix pharmaceuticals and was in clinical phase 2, but now it has been terminated.
1.Unexpected finding of delayed-onset seizures in HIV-positive, treatment-experienced subjects in the Phase IIb evaluation of fosdevirine (GSK2248761).
Margolis DA1, Eron JJ, DeJesus E, White S, Wannamaker P, Stancil B, Johnson M. Antivir Ther. 2014;19(1):69-78. doi: 10.3851/IMP2689. Epub 2013 Oct 24.
BACKGROUND: Fosdevirine (GSK2248761) is a non-nucleoside reverse transcriptase inhibitor with HIV-1 activity against common efavirenz-resistant strains. Two partially blind, randomized, Phase IIb studies were initiated (1 in treatment-naive and 1 in treatment-experienced subjects with HIV) to select a once-daily dose of fosdevirine for Phase III trials.
2.Central nervous system disposition and metabolism of Fosdevirine (GSK2248761), a non-nucleoside reverse transcriptase inhibitor: an LC-MS and Matrix-assisted laser desorption/ionization imaging MS investigation into central nervous system toxicity.
Castellino S1, Groseclose MR, Sigafoos J, Wagner D, de Serres M, Polli JW, Romach E, Myer J, Hamilton B. Chem Res Toxicol. 2013 Feb 18;26(2):241-51. doi: 10.1021/tx3004196. Epub 2012 Dec 20.
The CNS disposition and metabolism of Fosdevirine (FDV), an HIV non-nucleoside reverse transcriptase inhibitor, was investigated in four patients who unexpectedly experienced seizures after at least 4 weeks of treatment in a Phase IIb, HIV-1 treatment experienced study. In addition, the CNS disposition and metabolism of FDV was examined in samples from rabbit, minipig, and monkey studies. LC-MS was used to characterize and estimate the concentrations of FDV and its metabolites in cerebral spinal fluid (seizure patients, rabbit, and monkey) and brain homogenate (rabbit, minipig, and monkey). The application of matrix-assisted laser desorption/ionization imaging mass spectrometry (MALDI IMS) provided the spatial distribution of FDV and its metabolites in brain tissue (rabbit, minipig, and monkey). A cysteine conjugate metabolite resulting from an initial glutathione (GSH) Michael addition to the trans-phenyl acrylonitrile moiety of FDV was the predominant drug-related component in the samples from seizure patients, rabbits, and minipigs.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related NNRTIs Products


Fosdevirine
(CAS: 1018450-26-4)

Fosdevirine is a highly potent next-generation Anti-HIV nonnucleoside reverse transcriptase inhibitor (NNRTI) with an EC50 of 11 nM. It is a novel and once-dail...

CAS 1097733-15-7 IDX899

IDX899
(CAS: 1097733-15-7)

IDX899 is a novel next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) with activity against efavirenz-resistant strains. It is used in the tre...

Etravirine D4
(CAS: 1142095-93-9)

The labeled form of Etravirine, is an inhibitor of HIV reverse transcriptase, could be used in the treatment of HIV infection.

CAS 700361-47-3 Rilpivirine HCl

Rilpivirine HCl
(CAS: 700361-47-3)

Rilpivirine, also known as TMC278, is a drug used as part of antiretroviral therapy (ART). Rilpivirine is a second-generation non-nucleoside reverse transcripta...

CP-94707
(CAS: 343250-05-5)

CP-94707 is a new nonnucleoside reverse transcriptase inhibitor (NNRTI).

Quick Inquiry

Verification code

Featured Items