A CCR3 antagonist (IC50 = 4.5 nM in a radioligand binding assay); selective for CCR3 over CXCR1

SB-328437 – 10 mg

Brand:
Cayman
CAS:
247580-43-4
Storage:
-20
UN-No:
Non-Hazardous - /

SB-328437 is a nonpeptide chemokine (C-C motif) receptor 3 (CCR3) antagonist (IC50 = 4.5 nM in a radioligand binding assay).{32621} It is selective for CCR3 over chemokine (C-X-C motif) receptor 1 (CXCR1), CXCR2, CCR7, complement 3a receptor (C3aR), and C5aR (IC50s = >27, >27, >33, >10, and >10 µM, respectively). SB-328437 (3.3-1,000 nM) inhibits calcium mobilization induced by chemokine (C-C motif) ligand 11 (CCL11), CCL24, and CCL13 in RBL-2H3-CCR3 cells and eosinophils. In vivo, SB-328437 reduces pulmonary Ccr3 mRNA expression, the number of eosinophils and monocytes in bronchoalveolar lavage fluid (BALF), and pulmonary IL-4 and TNF-α levels in a mouse model of asthma.{49498}  

 

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Description

A CCR3 antagonist (IC50 = 4.5 nM in a radioligand binding assay); selective for CCR3 over CXCR1, CXCR2, CCR7, C3aR, and C5aR (IC50s = >27, >27, >33, >10, and >10 µM, respectively); inhibits calcium mobilization induced by C-C motif ligand 11 CCL11, CCL24, and CCL13 in RBL-2H3-CCR3 cells and eosinophils from 3.3-1,000 nM; reduces pulmonary Ccr3 mRNA expression, the number of eosinophils and monocytes in BALF, and pulmonary IL-4 and TNF-α levels in a mouse model of asthma

Formal name: N-(1-naphthalenylcarbonyl)-4-nitro-L-phenylalanine, methyl ester

Synonyms: 

Molecular weight: 378.4

CAS: 247580-43-4

Purity: ≥98%

Formulation: A crystalline solid

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