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Chemical Structure : AMG487
CAS No.: 473719-41-4
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | $528 | In stock | |
| 100 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 603.60 | |
| Formula | C32H28F3N5O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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