Cabotegravir (GSK744; GSK1265744)

Alias: GSK744; S/GSK 1265744; GSK-744; S/GSK1265744; GSK 744; S/GSK-1265744; Cabotegravir; Cabenuva.
Cat No.:V1835 Purity: ≥98%
Cabotegravir (formerly GSK744; GSK1265744; GSK-744; GSK-1265744;Rekambys; Cabenuva) is a potent, orally bioavailable and long-acting inhibitor of HIV integrase approved in 2020 for the treatment and prevention of HIV infection.
Cabotegravir (GSK744; GSK1265744) Chemical Structure CAS No.: 1051375-10-0
Product category: Reverse Transcriptase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
100mg
250mg
Other Sizes

Other Forms of Cabotegravir (GSK744; GSK1265744):

  • Dolutegravir (GSK1349572)
  • Cabotegravir Sodium
  • Cabotegravir-d5
Official Supplier of:
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Top Publications Citing lnvivochem Products
InvivoChem's Cabotegravir (GSK744; GSK1265744) has been cited by 1 publication
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Cabotegravir (formerly GSK744; GSK1265744; GSK-744; GSK-1265744; Rekambys; Cabenuva) is a potent, orally bioavailable and long-acting inhibitor of HIV integrase approved in 2020 for the treatment and prevention of HIV infection. The combination of cabotegravir and rilpivirine (Cabenuva) was also approved in 2021 for HIV treatment. cabotegravir has a broad spectrum of activity against different HIV subtypes. Cabotegravir inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. In resistance passage experiments, integrase enzyme assays, and cellular assays with site-directed molecular (SDM) HIV clones resistant to other classes of anti-HIV-1 agents and earlier integrase strand transfer inhibitors, Cabotegravir showed efficient inhibition of HIV replication through inhibiting HIV integrase. It is an investigational new drug under development for the treatment of HIV infection.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
With an IC50 of 3.0 nM, capetreavir (GSK-1265744) blocks the strand transfer reaction that HIV-1 integrase catalyzes in vitro. In PBMCs, the antiviral EC50 against NL432 and HIV-1 Ba-L was 0.34 nM and 0.22 nM, respectively. The EC50 in MT-4 cells was found to be 0.57 nM using CellTiter-Glo, 1.3 nM using MTT, and 0.5 nM in the pseudotyped self-inactivating virus (PHIV) test [3].
ln Vivo
In mice, capetreavir can have a half-life of up to 54 days [1]. When macaques (Macaques) are infected with SIVmac251, they are protected by capetregravir (iv; single dose or twice; 25 or 50 mg/kg) [4].
Cell Assay
Cell Viability Assay[3]
Cell Types: MT-4 cells
Tested Concentrations: 0-32 nM
Incubation Duration: 4 or 5 days
Experimental Results: demonstrated antiviral activity with an EC50 of 1.3 nM.
Animal Protocol

In female pigtail macaques model that intravaginal inoculated simian/human immunodeficiency virus twice a week for up to 11 weeks, GSK744 injection prevented the macaques from being infected by virus while placebo controls were infected after a 4 median vaginal challenges with SHIV which reminded that GSK744 may be a potential preexposure prophylaxis drug for prevention via inhibiting HIV integrase
References
[1]. Zhou T, et al. Creation of a nanoformulated cabotegravir prodrug with improved antiretroviral profiles. Biomaterials. 2018 Jan;151:53-65.
[2]. Reese MJ, et al. Drug interaction profile of the HIV integrase inhibitor cabotegravir: assessment from in vitro studies and a clinical investigation with midazolam. Xenobiotica. 2015 Sep 4:1-12.
[3]. Yoshinaga T, et al. Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection. Antimicrob Agents Chemother. 2015 Jan;59(1):397-406.
[4]. Andrews CD, et al. Cabotegravir long acting injection protects macaques against intravenous challenge with SIVmac251. AIDS. 2017 Feb 20;31(4):461-467.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H17F2N3O5
Molecular Weight
405.35
CAS #
1051375-10-0
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
Chemical Name
(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
Synonyms
GSK744; S/GSK 1265744; GSK-744; S/GSK1265744; GSK 744; S/GSK-1265744; Cabotegravir; Cabenuva.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 38 mg/mL (93.7 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4670 mL 12.3350 mL 24.6700 mL
5 mM 0.4934 mL 2.4670 mL 4.9340 mL
10 mM 0.2467 mL 1.2335 mL 2.4670 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Cabotegravir (GSK744, GSK1265744)

    Effects of inhibitors on various forms of viral DNA were evaluated separately with HIV-1 NL432-infected MT-4 cells to determine the amounts of integrated viral DNA (a), 2-LTR circular viral DNA (b), or total viral DNA (c). Antimicrob Agents Chemother. 2015 Jan;59(1):397-406.
  • Cabotegravir (GSK744, GSK1265744)

    Long-term culture of infected MT-2 cells with escalating concentrations of INSTIs. Antimicrob Agents Chemother. 2015 Jan;59(1):397-406.
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