GS-9770 | HIV-1 protease inhibitor | Probechem Biochemicals

Chemical Structure : GS-9770

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GS-9770 (GS9770)

货号: PC-21801Not For Human Use, Lab Use Only.

GS-9770 is a potent, selective, non-peptidomimetic and orally active HIV protease inhibitor with Ki(app) value of 0.16 nM (recombinant HIV-1 PR).

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生物&药学活性

GS-9770 is a potent, selective, non-peptidomimetic and orally active HIV protease inhibitor with Ki(app) value of 0.16 nM (recombinant HIV-1 PR).
GS-9770 substantially reduces Gag polyprotein cleavage and the concomitant release of mature p24 protein at 10 nM, with complete inhibition of p24 formation at 100 nM in virus-producing HEK293T cells.
GS-9770 shows high antiviral potency identical to that of atazanavir (ATV), with a mean 50% effective concentration (EC50) value of 11 nM for MT-4 cells acutely infected with the syncytia-inducing HIV-1 IIIb strain.
GS-9770 exhibitsmean EC50 value of 8.5 nM in primary human immune target cells acutely infected with HIV-1 BaL strain using a virus (p24) production assay.
GS-9770 maintainshigh antiviral potency (EC50 range of 1.9 to 26 nM) against HIV-1 and HIV-2.
Combinations of GS-9770 with the NRTIs tenofovir alafenamide (TAF) or FTC, the NNRTI rilpivirine (RPV), the INSTI bictegravir (BIC), or the capsid inhibitor lenacapavir (LEN) resulted in highly synergistic anti-HIV activity with mean synergy volumes ranging from 163 to 180 µM.

物理化学性质&存储条件

分子量	811.16
分子式	C35H34ClF7N10O3
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	(2S)-2-[(4R)-2-Amino-4-[4-(2-cyclopropyl-2H-1,2,3-triazol-4-yl)phenyl]-4,5-dihydro-5-oxo-4-(3,3,3-trifluoro-2,2-dimethylpropyl)-1H-imidazol-1-yl]-2-[4-chloro-3-[1-(difluoromethyl)-1H-1,2,4-triazol-5-yl]phenyl]ethyl N-[1-(difluoromethyl)cyclopropyl]carbamate

参考文献

1. Andrew Mulato, et al. Antimicrob Agents Chemother. 2024 Feb 21:e0137323.

GS-9770 (GS9770)

生物&药学活性

物理化学性质&存储条件

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GS-9770 (GS9770)

生物&药学活性

物理化学性质&存储条件

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