SML3153

AMG 487

≥98% (HPLC)

• Synonym(e): (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
• Empirische Formel (Hill-System): C₃₂H₂₈F₃N₅O₄
• CAS-Nummer: 473719-41-4
• Molekulargewicht: 603.59
• MDL-Nummer: MFCD30536209
• UNSPSC-Code: 12352200
• NACRES: NA.51

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 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)
• InChIKey: IEKPMGNVFDUVPK-UHFFFAOYSA-N

Beschreibung

Biochem./physiol. Wirkung

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.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable