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Biochem/physiol Actions
AMG 487 is an orally available, potent and selective chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (IC50 = 8/8.2 nM against CXCL10/11 (IP-10/ITAC) for CXCR3 binding) that inhibits CXCR3 ligands-induced cell migration (CXCL10/11/9 IC50 = 8/15/36 nM). AMG 487 inhibits ITAC-induced calcium mobilization in vitro (IC50 = 5 nM) and reduces bleomycin-induced cellular lung recruitment in wild-type mice to the same level as in Cxcr3-deficient mice in vivo (3 mg/kg b.i.d. s.c.).
Orally available, potent and selective chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist in vitro and in vivo.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | FC(F)(F)Oc1ccc(cc1)CC(=O)N(Cc5cnccc5)C(=C2Nc3ncccc3C(=O)N2c4ccc(cc4)OCC)C |
| InChI | 1S/C32H28F3N5O4/c1-3-43-25-14-10-24(11-15-25)40-30(38-29-27(31(40)42)7-5-17-37-29)21(2)39(20-23-6-4-16-36-19-23)28(41)18-22-8-12-26(13-9-22)44-32(33,34)35/h4-17,19H,3,18,20H2,1-2H3,(H,37,38) |
| InChI key | IEKPMGNVFDUVPK-UHFFFAOYSA-N |
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