A CXCR3 antagonist (IC50 = 8.2 nM in a radioligand binding assay); inhibits CXCL10-

AMG 487 – 10 mg

Brand:
Cayman
CAS:
473719-41-4
Storage:
-20
UN-No:
Non-Hazardous - /

AMG 487 is a chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (IC50 = 8.2 nM in a radioligand binding assay).{50088} It inhibits cell migration induced by chemokine (C-X-C motif) ligand 10 (CXCL10), CXCL11, and CXCL9 (IC50s = 8, 15, and 36 nM, respectively). In vivo, AMG 487 (3 mg/kg) inhibits bronchoalveolar lavage fluid (BALF) cell infiltration in a mouse model of bleomycin-induced cellular recruitment. It reduces the number of lung metastases in the K7M2 and Saos-LM7 osteosarcoma mouse xenograft models.{47785} AMG 487 (5 mg/kg) also restores mitochondrial function and inhibits mitochondrial-dependent hepatocellular apoptosis in a mouse model of non-alcoholic steatohepatitis (NASH).{47786}  

 

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Description

A CXCR3 antagonist (IC50 = 8.2 nM in a radioligand binding assay); inhibits CXCL10-, CXCL11-, and CXCL9-induced cell migration (IC50s = 8, 15, and 36 nM, respectively); inhibits BALF cell infiltration in a mouse model of bleomycin-induced cellular recruitment at 3 mg/kg; reduces the number of lung metastases in the K7M2 and Saos-LM7 osteosarcoma mouse xenograft models; restores mitochondrial function and inhibits mitochondrial-dependent hepatocellular apoptosis in a mouse model of NASH at 5 mg/kg

Formal name: N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)-benzeneacetamide

Synonyms: 

Molecular weight: 603.6

CAS: 473719-41-4

Purity: ≥98%

Formulation: A crystalline solid

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