SML3153
AMG 487
≥98% (HPLC)
Synonym(s):
(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, AMG-487, AMG487
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About This Item
Empirical Formula (Hill Notation):
C32H28F3N5O4
CAS Number:
Molecular Weight:
603.59
UNSPSC Code:
12352200
NACRES:
NA.51
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
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
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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