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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-BMS-639623
BMS-639623

Chemical Structure : BMS-639623

CAS No.: 675122-44-8

BMS-639623 (BMS 639623)

货号: PC-20730Not For Human Use, Lab Use Only.

BMS-639623 is a potent, selective and orally bioavailable CCR3 antagonist with binding IC50 of 0.3 nM and chemotaxis IC50 of 0.04 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BMS-639623 is a potent, selective and orally bioavailable CCR3 antagonist with binding IC50 of 0.3 nM and chemotaxis IC50 of 0.04 nM.
BMS-639623 is selective against other 7TM receptors and ion channels.
BMS-639623 also shows activity in eotaxin-stimulated calcium flux in eosinophils with IC50 of 0.87 nM.
BMS-639623 shows poor binding and chemotaxis inhibition potency in the mouse (IC50=31, 870 nM, respectively).
BMS-639623 inhibits cyno eosinophil chemotaxis with IC50 of 0.15 nM.
BMS-639623 (5 mg/kg b.i.d.) reduces the allergen-dependent eosinophilia by 65%, 78%, and 82% in cyno study.

物理化学性质&存储条件

分子量 481.58
分子式 C25H32FN7O2
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(NC1=CC=CC(C2=NN=NN2C)=C1)N[C@@H]([C@@H](O)CN3C[C@H](CC4=CC=C(F)C=C4)CCC3)C

参考文献

1. Gardner DS, et al. Bioorg Med Chem Lett. 2008 Jan 15;18(2):586-95.

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