PF-07054894 | CCR6 inhibitor | Probechem Biochemicals

Chemical Structure : PF-07054894

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PF-07054894 (PF 07054894)

货号: PC-20761Not For Human Use, Lab Use Only.

PF-07054894 is a potent, functionally selective CCR6 antagonist, blocks in vitro CCL20- dependent human T cell chemotaxis with IC50 of 5.7 nM.

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生物&药学活性

PF-07054894 is a potent, functionally selective CCR6 antagonist, blocks in vitro CCL20- dependent human T cell chemotaxis with IC50 of 5.7 nM.
PF-07054894 dispays negligible activity (<12% over basal activity) in an assay panel of 168 G protein-coupled receptors, with more than 30% inhibition of agonist-dependent activity on only 3 receptors: CCR6, CCR7, and CXCR2.
PF-07054894 displays >50- and 150-fold functional selectivity relative to CCR7 and CXCR2.
PF-07054894 increased the frequency of CCR6+ peripheral blood T cells suggesting that blockade of CCR6 inhibited homeostatic migration of T cells from blood to tissues of naïve cynomolgus monkeys.
PF-07054894 caused an increase in cell surface CCR6 in mouse and monkey B cells which was recapitulated in mouse splenocytes in vitro.

物理化学性质&存储条件

分子量	466.54
分子式	C24H30N6O4
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-((2-(((1,4-dimethyl-1H-pyrazol-3-yl)(1-methylcyclopentyl)methyl)amino)-3,4-dioxocyclobut-1-en-1-yl)amino)-3-hydroxy-N,N-dimethylpicolinamide

参考文献

1. Wei Li, et al. J Pharmacol Exp Ther. 2023 May 4;JPET-AR-2022-001452.

PF-07054894 (PF 07054894)

生物&药学活性

物理化学性质&存储条件

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PF-07054894 (PF 07054894)

生物&药学活性

物理化学性质&存储条件

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