Cabotegravir sodium - 99%, high purity , Human immunodeficiency virus type 1 integrase inhibitor, CAS No.1051375-13-3, Human immunodeficiency virus type 1 integrase inhibitor
Cabotegravir sodium - 99%, high purity , Human immunodeficiency virus type 1 integrase inhibitor, CAS No.1051375-13-3, Human immunodeficiency virus type 1 integrase inhibitor
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 IC 50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIV ADA , OAT3 and OAT1, respecti
Storage Temp
Store at 2-8°C,Desiccated
Shipped In
Wet ice
Action Type
INHIBITOR
Mechanism of action
Human immunodeficiency virus type 1 integrase inhibitor
Product Description
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 IC 50 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
In Vitro
Cabotegravir (GSK-1265744) inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC 50 of 3.0 nM in vitro. The antiviral EC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MT-4 cells Concentration: 0-32 nM Incubation Time: 4 or 5 days Result: Showed antiviral activity with an EC 50 of 1.3 nM.
In Vivo
The half-life of Cabotegravir is up to 54 days in mice . Cabotegravir (25 or 50 mg/kg; i.v.; single dose or twice) protects Macaques against intravenous challenge with SIVmac251. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:IC 50 : 2.5 nM (HIV ADA ), IC 50 : 0.41 μM (OAT3), 0.81 μM (OAT1)
