Cabotegravir sodium  (Synonyms: GSK-1265744 sodium; S/GSK1265744 sodium)

Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC₅₀ values of 2.5 nM, 0.41 μM and 0.81 μM for HIV_ADA, OAT3 and OAT1, respectively. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir sodium can be used to research AIDS^[1][2].

IC₅₀: 2.5 nM (HIV_ADA)^[1]
IC₅₀: 0.41 μM (OAT3), 0.81 μM (OAT1)^[2]

Cabotegravir (GSK-1265744) inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC₅₀ of 3.0 nM in vitro. The antiviral EC₅₀ against HIV-1 Ba-L is 0.22 nM and that against NL432 is 0.34 nM in PBMCs, 0.57 nM using CellTiter-Glo and 1.3 nM using MTT in MT-4, and 0.5 nM in the PHIV assay, which uses a pseudotyped self-inactivating virus^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

The half-life of Cabotegravir is up to 54 days in mice^[1].
Cabotegravir (25 or 50 mg/kg; i.v.; single dose or twice) protects Macaques against intravenous challenge with SIVmac251^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

427.33

C₁₉H₁₆F₂N₃NaO₅

1051375-13-3

Solid

White to off-white

FC1=C(CNC(C2=CN3C(C(N([C@@H](C)CO4)[C@@]4([H])C3)=O)=C(O[Na])C2=O)=O)C=CC(F)=C1

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Zhou T, et al. Creation of a nanoformulated cabotegravir prodrug with improved antiretroviral profiles. Biomaterials. 2018 Jan;151:53-65.  [Content Brief]

  [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. 2016;46(5):445-56.  [Content Brief]

  [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.  [Content Brief]

  [4]. Andrews CD, et al. Cabotegravir long acting injection protects macaques against intravenous challenge with SIVmac251. AIDS. 2017 Feb 20;31(4):461-467.  [Content Brief]