GSK3640254 (GSK254, Fipravirimat)

Chemical Structure : GSK3640254

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货号: PC-72601Not For Human Use, Lab Use Only.

GSK3640254 (GSK254, Fipravirimat) is a novel potent HIV-1 maturation inhibitor with EC90 of 33 nM against a minilibrary of clinically relevant HIV-1 polymorphisms in a multiple-cycle assay.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

GSK3640254 (GSK254, Fipravirimat) is a novel potent HIV-1 maturation inhibitor with EC90 of 33 nM against a minilibrary of clinically relevant HIV-1 polymorphisms in a multiple-cycle assay.
GSK3640254 shows potent binding affinity for HIV-1 VLPs ( Kd=1.4 nM).
GSK3640254 displayed strong antiviral activity against a library of subtype B and C chimeric viruses containing Gag polymorphisms and site-directed mutants previously shown to affect potency of earlier-generation maturation inhibitors.
GSK3640254 exhibited robust antiviral activity against a panel of HIV-1 clinical isolates in PBMCs with a mean EC50 of 9 nM.
GSK3640254 inhibited cleavage of p25 in a range of polymorphic HIV-1 Gag VLPs.

物理化学性质&存储条件

分子量	727.077
分子式	C43H67FN2O4S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-4-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a-((2-(1,1-dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1H-cyclopenta[a]chrysen-9-yl)-1-(fluoromethyl)cyclohex-3-ene-1-carboxylic acid

参考文献

1. Dicker I, et al. Antimicrob Agents Chemother. 2022 Jan 18;66(1):e0187621.

2. Spinner CD, et al. Clin Infect Dis. 2022 Jan 6:ciab1065.

3. Pene Dumitrescu T, et al. Br J Clin Pharmacol. 2021 Aug 24.

4. Pene Dumitrescu T, Antimicrob Agents Chemother. 2021 May 18;65(6):e02173-20.