Name: BX 471
Price: 320.00 USD

- Overview
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    Background
    
    Ki: 1 nM to 5.5 nMThe CC chemokine receptor-1 (CCR1) is a prime therapeutic target for treating autoimmune diseases. BX 471 is a potent, selective, and orally active antagonist of the CC Chemokine Receptor-1.In vitro: Competition binding studies revealed that BX 471 was able to displace the CCR1 ligands macrophage inflammatory protein-1a, RANTES, and monocyte chemotactic protein-3 with high affinity. BX 471 was a potent functional antagonist based on its ability to inhibit plenty of CCR1-mediated effects. BX 471 also demonstrated a greater than 10,000-fold selectivity for CCR1 compared with 28 G-protein-coupled receptors [1]. In vivo: Pharmacokinetic studies demonstrated that BX 471 was orally active with a 60% bioavailability in dogs. Furthermore, in a rat experimental allergic encephalomyelitis model of multiple sclerosis, BX 471 effectively reduces disease [1]. Clinical trial: Up to now, BX 471 is still in the preclinical development stage.
- Properties
  - Categories
    
    CCR1 antagonist, potent and selective
    
    Alternative Name
    
    (R)-1-(5-chloro-2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-1-yl)-2-oxoethoxy)phenyl)urea
    
    CAS Number
    
    217645-70-0
    
    Molecular Formula
    
    C21H24ClFN4O3
    
    Molecular Weight
    
    434.89
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥136.8 mg/mL in DMSO; ≥26.9 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    ClC1=CC=C(C(NC(N)=O)=C1)OCC(N2[[email protected]](C)CN(CC(C=C3)=CC=C3F)CC2)=O
    
    * For Research Use Only