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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-YM-355179
YM-355179

Chemical Structure : YM-355179

CAS No.: 672957-37-8

YM-355179 (YM355179)

货号: PC-20725Not For Human Use, Lab Use Only.

YM-355179 is a potent selective, and orally available antagonist of CC chemokine receptor 3 (CCR3) with binding IC50 of 7.6 nM (CCL5).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

YM-355179 is a potent selective, and orally available antagonist of CC chemokine receptor 3 (CCR3) with binding IC50 of 7.6 nM (CCL5).
YM-355179 did not affect the binding of CCL5 to CCR1 or CCR5.
YM-355179 inhibited CCL11-induced, intracellular Ca(2+) influx, chemotaxis, and eosinophil degranulation with IC(50) values of 8.0, 24, and 29 nM, respectively.
YM-355179 did not affect any CC chemokine receptor (CCR1, CCR2, CCR4, or CCR5)-mediated Ca(2+) influx signals.
YM-355179 (1 mg/kg, oral) inhibited CCL11-induced shape change of whole blood eosinophils in cynomolgus monkeys.
YM-355179 (1 mg/kg, i.v.) also inhibited eosinophil infiltration into airways of cynomolgus monkeys after segmental bronchoprovocation with CCL11.

物理化学性质&存储条件

分子量 502.59
分子式 C29H31FN4O3
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@H]1CN(CC2=CC=C3C=C(F)C=CC3=C2)CC1)/C=C4CCN(C(C5=NC=C(C)C=C5O)=O)CC\4

参考文献

1. Tatsuaki Morokata, et al. J Pharmacol Exp Ther. 2006 Apr;317(1):244-50.

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