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Cabotegravir CAS: 1051375-10-0

Category: Inhibitors
Product Name: Cabotegravir
Cat No: I000281
CAS No: 1051375-10-0
Synonyms: (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
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
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
Solubility: DMSO: ≥ 12.67 mg/mL
Target: HIV Integrase
IC50: 0.81 μM (OAT1), 0.41 μM (OAT3) [1]
Storage: Store at -20°C
CAS 1051375-10-0,Cabotegravir
  • Description

Cabotegravir 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).
IC50 value: 0.81 μM (OAT1), 0.41 μM (OAT3) [1]
Target: OAT1, OAT3
Cabotegravir is a potent HIV integrase inhibitor in clinical development as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection.[2] Cabotegravir is an HIV-1 integrase inhibitor under development as a tablet for both oral lead-in therapy and long-acting (LA) injectable for intramuscular dosing.[3]

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References

1:Lack of effect of oral cabotegravir on the pharmacokinetics of a levonorgestrel/ethinyl oestradiol-containing oral contraceptive in healthy adult women. Trezza C, Ford SL, Gould E, Lou Y, Huang C, Ritter JM, Buchanan AM, Spreen W, Patel P.Br J Clin Pharmacol. 2017 Jan 14. doi: 10.1111/bcp.13236. [Epub ahead of print] PMID: 28087972
2:Cabotegravir long acting injection protects macaques against intravenous challenge with SIVmac251. Andrews CD, Bernard LS, Poon AY, Mohri H, Gettie N, Spreen WR, Gettie A, Russell-Lodrigue K, Blanchard J, Hong Z, Ho DD, Markowitz M.AIDS. 2017 Feb 20;31(4):461-467. doi: 10.1097/QAD.0000000000001343. PMID: 27902508
3:Profile of cabotegravir and its potential in the treatment and prevention of HIV-1 infection: evidence to date. Whitfield T, Torkington A, van Halsema C.HIV AIDS (Auckl). 2016 Oct 14;8:157-164. eCollection 2016. Review. PMID: 27799824 Free PMC Article
4:Effect of Cabotegravir on Cardiac Repolarization in Healthy Subjects. Lou Y, Buchanan AM, Chen S, Ford SL, Gould E, Margolis D, Spreen WR, Patel P.Clin Pharmacol Drug Dev. 2016 Nov;5(6):509-516. doi: 10.1002/cpdd.272. Epub 2016 Jun 22. PMID: 27162089 Free PMC Article
5:Interspecies scaling of excretory amounts using allometry - retrospective analysis with rifapentine, aztreonam, carumonam, pefloxacin, miloxacin, trovafloxacin, doripenem, imipenem, cefozopran, ceftazidime, linezolid for urinary excretion and rifapentine, cabotegravir, and dolutegravir for fecal excretion. Srinivas NR.Xenobiotica. 2016 Sep;46(9):784-92. doi: 10.3109/00498254.2015.1121554. Epub 2015 Dec 29. PMID: 26711252
6:Drug interaction profile of the HIV integrase inhibitor cabotegravir: assessment from in vitro studies and a clinical investigation with midazolam. Reese MJ, Bowers GD, Humphreys JE, Gould EP, Ford SL, Webster LO, Polli JW.Xenobiotica. 2016;46(5):445-56. doi: 10.3109/00498254.2015.1081993. Epub 2015 Sep 4. PMID: 26340566
7:Cabotegravir plus rilpivirine, once a day, after induction with cabotegravir plus nucleoside reverse transcriptase inhibitors in antiretroviral-naive adults with HIV-1 infection (LATTE): a randomised, phase 2b, dose-ranging trial. Margolis DA, Brinson CC, Smith GH, de Vente J, Hagins DP, Eron JJ, Griffith SK, St Clair MH, Stevens MC, Williams PE, Ford SL, Stancil BS, Bomar MM, Hudson KJ, Smith KY, Spreen WR; LAI116482 Study Team..Lancet Infect Dis. 2015 Oct;15(10):1145-55. doi: 10.1016/S1473-3099(15)00152-8. Epub 2015 Jul 19. PMID: 26201299
8:Disposition and metabolism of cabotegravir: a comparison of biotransformation and excretion between different species and routes of administration in humans. Bowers GD, Culp A, Reese MJ, Tabolt G, Moss L, Piscitelli S, Huynh P, Wagner D, Ford SL, Gould EP, Pan R, Lou Y, Margolis DA, Spreen WR.Xenobiotica. 2016;46(2):147-62. doi: 10.3109/00498254.2015.1060372. Epub 2015 Jul 1. PMID: 26134155
9:Cabotegravir long-acting for HIV-1 prevention. Andrews CD, Heneine W.Curr Opin HIV AIDS. 2015 Jul;10(4):258-63. doi: 10.1097/COH.0000000000000161. Review. PMID: 26049951
10:Formulation and pharmacology of long-acting cabotegravir. Trezza C, Ford SL, Spreen W, Pan R, Piscitelli S.Curr Opin HIV AIDS. 2015 Jul;10(4):239-45. doi: 10.1097/COH.0000000000000168. Review. PMID: 26049948

price inquiry for CAS:1051375-10-0, Product:Cabotegravir