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GSK3532795

Cat. No. M28313
GSK3532795 Structure
Synonym:

BMS-955176

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Biological Activity

GSK3532795 (BMS-955176) is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively.

Chemical Information
Molecular Weight 691.02
Formula C42H62N2O4S
CAS Number 1392312-45-6
Form Solid
Storage Powder -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jacob J Swidorski, et al. Bioorg Med Chem Lett. Design and exploration of C-3 benzoic acid bioisosteres and alkyl replacements in the context of GSK3532795 (BMS-955176) that exhibit broad spectrum HIV-1 maturation inhibition

[2] Ira Dicker, et al. PLoS One. Resistance profile of the HIV-1 maturation inhibitor GSK3532795 in vitro and in a clinical study

[3] Javier Morales-Ramirez, et al. PLoS One. Safety, efficacy, and dose response of the maturation inhibitor GSK3532795 (formerly known as BMS-955176) plus tenofovir/emtricitabine once daily in treatment-naive HIV-1-infected adults: Week 24 primary analysis from a randomized Phase IIb trial

[4] Alicia Regueiro-Ren, et al. J Med Chem. Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1䲧瘀Ỵ瘁㧀痿羹皘的ࡍţࡍĀ�皚嶁皖Ѐ瑖犤䀹ࡀࡍĀꃨࡀ彿犥奋犥巫犥ࡀԨࡁ彿犥Ԝࡁ塚犥Ԩࡁꍈ犪ࡀ學犥漸犪圔犥ࡀ圞犥圭犥䀹魸皞ţ ţ憠癴Š얨څ

[5] Neelanjana Ray, et al. J Acquir Immune Defic Syndr. The Second-Generation Maturation Inhibitor GSK3532795 Maintains Potent Activity Toward HIV Protease Inhibitor-Resistant Clinical Isolates

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Keywords: GSK3532795, BMS-955176 supplier, HIV Protease, inhibitors, activators


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