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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-AMG487
AMG487

Chemical Structure : AMG487

CAS No.: 473719-41-4

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AMG487 (AMG-487, VUF10085)

货号: PC-20733Not For Human Use, Lab Use Only.

AMG487 (AMG 487, VUF10085) is a potent and selective orally bioavailable chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist with IC50 of 8 nM for inhibiting 125I-IP-10 binding.

规格 价格 库存 数量
5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3480 In stock
50 mg ￥5480 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AMG487 (AMG 487, VUF10085) is a potent and selective orally bioavailable chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist with IC50 of 8 nM for inhibiting 125I-IP-10 binding.
AMG 487 also inhibits binding of 125I-ITAC to CXCR3 with an IC50 value of 8.2 nM.
AMG487 inhibits CXCR3-mediated cell migration by the three CXCR3 chemokines (IP-10 IC50 = 8 nM, ITAC IC50 = 15 nM, and MIG IC50 = 36 nM).
AMG487 inhibits calcium mobilization in response to ITAC (IC50 = 5 nM).
AMG487 exhibits good potency in binding and functional assays and good in vivo pharmacokinetic properties across species. AMG487 is a potent inhibitor of cellular recruitment in vivo using a bleomycine-mouse model.

物理化学性质&存储条件

分子量 603.60
分子式 C32H28F3N5O4
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)-N-{1-[3-(4-Ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]-pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxyphenyl)-acetamide

参考文献

1. Verzijl D, et al. J Pharmacol Exp Ther. 2008 May;325(2):544-55.et al.

2. Johnson M, et al. Bioorg Med Chem Lett. 2007;17:3339–3343.

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