A selective

BX 471 – 10 mg

Brand:
Cayman
CAS:
217645-70-0
Storage:
-20
UN-No:
Non-Hazardous - /

The CC chemokine receptor-1 (CCR1), whose ligands include macrophage inflammatory protein-1α (MIP-1α), RANTES, and monocyte chemotactic protein-3 (MCP-3), has a central role in leukocyte trafficking and is highly expressed in certain autoimmune diseases. BX 471 is a nonpeptide CCR1 antagonist that has been shown to displace MIP-1α, RANTES, and MCP-3 with Ki values of 1, 2.8, and 5.5 nM, respectively.{29906} It demonstrates >10,000-fold selectivity for CCR1 over 28 additional G protein-coupled receptors, including related chemokine receptors.{29906} In a rat experimental allergic encephalomyelitis model of multiple sclerosis, BX 471 at 50 mg/kg was shown to significantly reduce the severity of the disease.{29906} BX 471 also decreases the inflammatory response during sepsis, blocks migration of monocytes isolated from rheumatoid arthritis patients, and prevents macrophage and T-cell recruitment in a mouse model of lupus nephritis.{29904,29905,29903}  

 

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Description

A selective, nonpeptide CCR1 antagonist that can displace the endogenous CCR1 ligands, MIP-1α, RANTES, and MCP-3 with Ki values of 1, 2.8, and 5.5 nM, respectively; reduces chemotaxis of inflammatory cells in models of multiple sclerosis, sepsis, rheumatoid arthritis, and lupus nephritis

Formal name: N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-urea

Synonyms: 

Molecular weight: 434.9

CAS: 217645-70-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Autoimmunity|Lupus||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity|Sepsis/Shock

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