Cabotegravir


CAS No. : 1051375-10-0

Cabotegravir,1051375-10-0
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000281
Synonyms:GSK744; Cabotegravir; (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
Molecular Formula:C19H17F2N3O5
Molecular Weight:405.35
Target:HIV Integrase
IC50:0.81 μM (OAT1), 0.41 μM (OAT3)
Price:Get quote
We would like to match the lowest price on market if possible.

Your information is safe with us.

refresh
Appearance:Solid powder
Purity: > 98%
Cat No:I000281
Cas No:1051375-10-0
Product-Name:Cabotegravir
InChI:InChI=1S/C19H17F2N3O5/c1-9-8-29-14-7-23-6-12(16(25)17(26)15(23)19(28)24(9)14)18(27)22-5-10-2-3-11(20)4-13(10)21/h2-4,6,9,14,26H,5,7-8H2,1H3,(H,22,27)/t9-,14+/m0/s1
InChIKey:WCWSTNLSLKSJPK-LKFCYVNXSA-N
SMILES:C[C@H]1CO[C@H]2N1C(C3=C(O)C(C(C(NCC4=C(F)C=C(F)C=C4)=O)=CN3C2)=O)=O

Cabotegravir(cas 1051375-10-0), also known as GSK744, is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM). Cabotegravir is currently in Phase III trial for treatment of HIV infections.

Originator: Shionogi - GlaxoSmithKline (JV)
Developer: Gilead Sciences; National Institute of Allergy and Infectious Diseases; ViiV Healthcare
Class: Antiretrovirals; Fluorobenzenes; Oxazoles; Pyrazines; Pyridones; Small molecules
Mechanism of Action: HIV integrase inhibitors
Orphan Drug Status: No
1. Sci Transl Med. 2015 Jan 14;7(270):270ra5. doi: 10.1126/scitranslmed.3010297.
The long-acting integrase inhibitor GSK744 protects macaques from repeated intravaginal SHIV challenge.
Radzio J(1), Spreen W(2), Yueh YL(2), Mitchell J(1), Jenkins L(1), García-Lerma JG(3), Heneine W(1).
Author information:
(1)Laboratory Branch, Division of HIV/AIDS Prevention, National Center for HIV/AIDS, Viral Hepatitis, STD, and TB Prevention, Centers for Disease Control and Prevention, Atlanta, GA 30329, USA. (2)GlaxoSmithKline, Research Triangle Park, NC 27709, USA. (3)Laboratory Branch, Division of HIV/AIDS Prevention, National Center for HIV/AIDS, Viral Hepatitis, STD, and TB Prevention, Centers for Disease Control and Prevention, Atlanta, GA 30329, USA. ggarcia-lerma@cdc.gov.
Daily preexposure prophylaxis (PrEP) with Truvada is a proven HIV prevention strategy; however, its effectiveness is limited by low adherence. Antiretroviral drug formulations that require infrequent dosing may increase adherence and thus PrEP effectiveness. We investigated whether monthly injections of a long-acting formulation of the HIV integrase inhibitor GSK1265744 (GSK744 LA) prevented simian/human immunodeficiency virus (SHIV) infection by vaginal challenge in macaques. Female pigtail macaques (n = 12) were exposed to intravaginal inoculations of SHIV twice a week for up to 11 weeks. Half of the animals received a GSK744 LA injection every 4 weeks, and half received placebo. GSK744 LA, at plasma concentrations achievable with quarterly injections in humans, protected all six macaques from infection. Placebo controls were all infected after a median of 4 (range, 2 to 20) vaginal challenges with SHIV. Efficacy was related to high and sustained vaginal and plasma drug concentrations that remained above the protein-adjusted 90% inhibitory concentration during the dosing cycles. These data support advancement of GSK744 LA as a potential PrEP candidate for women.
Related Products
  • CAS No. :729607-74-3
    Product Name:

    BMS-707035

    Cat No: I004717 View details
  • CAS No. :518048-05-0
    Product Name:

    Raltegravir (MK-0518)

    Cat No: A000442 View details
  • CAS No. :1155419-89-8
    Product Name:

    BI 224436

    Cat No: I000568 View details
  • CAS No. :1051375-16-6
    Product Name:

    GSK1349572

    Cat No: A000782 View details