Chemical Structure : GSK812397
货号: PC-35088Not For Human Use, Lab Use Only.
GSK812397 is a potent, selective, noncompetitive, orally available antagonist of CXCR4 receptor, inhibits entry of X4-tropic strains of HIV-1 with IC50 of 4.60 nM and 1.50 nM in PBMCs and HOS assays, respectively.
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GSK812397 is a potent, selective, noncompetitive, orally available antagonist of CXCR4 receptor, inhibits entry of X4-tropic strains of HIV-1 with IC50 of 4.60 nM and 1.50 nM in PBMCs and HOS assays, respectively.
GSK812397 does not block CCR5-mediated viral entry in the R5 viral HOS assay (IC50>25 uM).
GSK812397 produces a concentration-dependent decrease in both an SDF-1-mediated chemotaxis and intracellular calcium release (IC50=0.34 nM and 2.41 nM, respectively) in cell-based functional assays.
GSK812397 demonstrates antiviral activity against a broad range of X4-utilizing strains of HIV-1.
分子量 | 420.561 | |
分子式 | C24H32N6O | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Jenkinson S, et al. Antimicrob Agents Chemother. 2010 Feb;54(2):817-24.
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