[CAS NO. 1051375-10-0]  Cabotegravir (GSK1265744)

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PRODUCTS SPECIFICATIONS [1051375-10-0]

Store
Catalog
SLK-S7766
Brand
Selleck
CAS
1051375-10-0

DESCRIPTION [1051375-10-0]

Overview

MDLMFCD25976748
Molecular Weight405.35
Molecular FormulaC19H17F2N3O5
SMILESO=C1C=2N(C[C@@]3(N1[C@@H](C)CO3)[H])C=C(C(NCC4=C(F)C=C(F)C=C4)=O)C(=O)C2O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.4670 mL12.3350 mL24.6700 mL
5 mM0.4934 mL2.4670 mL4.9340 mL
10 mM0.2467 mL1.2335 mL2.4670 mL
50 mM0.0493 mL0.2467 mL0.4934 mL

Description

Cabotegravir (GSK744, GSK1265744, S/GSK1265744) is a long-acting inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with of 3.0 nM. Phase 2.

Targets

HIV integrase [1]

In vitro

GSK1265744 inhibits HIV replication with EC50 of 0.22 nM and 0.34-1.3 nM against HIV-1 Ba-L and NL432, respectively. GSK1265744 produces cytotoxicity with CC50 of 6.4, 5.0, 9.2, and 13 μM in proliferating IM-9, U-937, MT-4, and Molt-4 cell lines, respectively.

In vivo

GSK1265744 (50 mg/kg) treatment protects rhesus macaques against three high-dose SHIV challenges.


Synonyms

Oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide, N-[(2,4-difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-, (3S,11aR)-
(3S,11aR)-N-[(2,4-Difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxooxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide
Cabotegravir
GSK 1265744A
GSK 744
(3s,11Ar)-n-(2,4-difluorobenzyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide