878197-98-9|GSK812397|(S)-(2-((methyl(5,6,7,8-tetrahydroquinolin-8-yl)amino)methyl)-5-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl)methanol|-范德生物科技公司

GSK812397

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names：
(S)-(2-((methyl(5,6,7,8-tetrahydroquinolin-8-yl)amino)methyl)-5-(4-methylpiperazin-1-yl)imidazo[1,2-a]pyridin-3-yl)methanol
CAS号：
878197-98-9
MDL Number：
MF(分子式)： C24H32N6O MW(分子量)： 420.56
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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FMK15840-100mg	100mg	>98%	¥ 0.00	¥ 0.00		Get quote	- +	¥ 0.00

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中文别名	GSK812397
英文别名	GSK812397; GSK-812397; GSK 812397.
CAS号	878197-98-9
Inchi	InChI=1S/C24H32N6O/c1-27-12-14-29(15-13-27)23-10-4-9-22-26-19(21(17-31)30(22)23)16-28(2)20-8-3-6-18-7-5-11-25-24(18)20/h4-5,7,9-11,20,31H,3,6,8,12-17H2,1-2H3/t20-/m0/s1
InchiKey	QUDMHFVRKBVGBY-FQEVSTJZSA-N
分子式 Formula	C24H32N6O
分子量 Molecular Weight	420.56
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	GSK812397(CAS:878197-98-9):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	GSK812397 is a potent entry inhibitor of X4-tropic strains of HIV-1, as demonstrated in multiple in vitro cellular assays. GSK812397 is a noncompetitive antagonist of the CXCR4 receptor, with GSK812397 producing a concentration-dependent decrease in both an SDF-1-mediated chemotaxis and intracellular calcium release (IC50s were 0.34+/-0.01 nM and 2.41+/-0.50 nM, respectively). GSK812397 is effective against a broad range of X4- and X4R5-utilizing clinical isolates. The potency and efficacy of GSK812397 are dependent on the individual isolate, with complete inhibition of infection observed with 24 of 30 isolates. GSK812397 does not show any detectable in vitro cytotoxicity and was highly selective for CXCR4. GSK812397 shows acceptable pharmacokinetic properties and bioavailability across species. GSK812397 has antiviral activity against a broad range of X4-utilizing strains of HIV-1 via a noncompetitive antagonism of the CXCR4 receptor.
Application1
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警示图
危险性	Warning
危险性警示
安全声明
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备注

[1]Planesas JM, Pérez-Nueno VI, Borrell JI, Teixidó J. Studying the bindinginteractions of allosteric agonists and antagonists of the CXCR4 receptor. J MolGraph Model. 2015 Jul;60:1-14. doi: 10.1016/j.jmgm.2015.05.004. Epub 2015 May 30.PubMed PMID: 26080355.

[2]Jenkinson S, Thomson M, McCoy D, Edelstein M, Danehower S, Lawrence W, WheelanP, Spaltenstein A, Gudmundsson K. Blockade of X4-tropic HIV-1 cellular entry byGSK812397, a potent noncompetitive CXCR4 receptor antagonist. Antimicrob AgentsChemother. 2010 Feb;54(2):817-24. doi: 10.1128/AAC.01293-09. Epub 2009 Nov 30.PubMed PMID: 19949058; PubMed Central PMCID: PMC2812144.

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