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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-PF-07054894
PF-07054894

Chemical Structure : PF-07054894

CAS No.: 2413693-96-4

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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

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

O=C(N(C)C)C1=NC=CC(NC2=C(N[C@@H](C3=NN(C)C=C3C)C4(C)CCCC4)C(C2=O)=O)=C1O

参考文献

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

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