Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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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. 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.
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].
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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].
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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. |
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Animal Protocol |
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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. |
Molecular Formula |
C19H17F2N3O5
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Molecular Weight |
405.35
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CAS # |
1051375-10-0
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Related CAS # |
Dolutegravir;1051375-16-6;Cabotegravir sodium;1051375-13-3;Cabotegravir-d5;2750534-77-9
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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
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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
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Synonyms |
GSK744; S/GSK 1265744; GSK-744; S/GSK1265744; GSK 744; S/GSK-1265744; Cabotegravir; Cabenuva.
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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)
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Solubility (In Vitro) |
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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.
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.