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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-YM-344031
YM-344031

Chemical Structure : YM-344031

CAS No.: 671204-98-1

YM-344031 (YM344031)

货号: PC-20726Not For Human Use, Lab Use Only.

YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM.
YM-344031 potently inhibits chemotaxis of human CCR3-expressing cells with IC50 of 19.9 nM.
YM-344031 (1-10mg/kg) orally administered to cynomolgus monkeys significantly inhibited Eotaxin-1-induced eosinophil shape change in whole blood.
YM-344031 (100mg/kg, oral) prevented both immediate- and late-phase allergic skin reactions in a mouse allergy model.
YM-344031 (50 mg/kg, b.i.d.) attenuated neurodegenerative pathologies and improves learning and memory performance in a mouse model of Alzheimer's disease, resulted in dramatic decreases in β-amyloid deposition, tau hyperphosphorylation and synaptic loss in the forebrain.

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=C(C)C=CC=[N+]5[O-])=O)CC\4

参考文献

1. Suzuki K, et al. Biochem Biophys Res Commun. 2006 Jan 27;339(4):1217-23.

2. Sui Y, et al. Brain Res. 2019 Sep 15;1719:1-10.

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