BX471 hydrochloride

CAS No. 288262-96-4

BX471 hydrochloride( BX-471 hydrochloride | BX 471 hydrochloride )

Catalog No. M13882 CAS No. 288262-96-4

BX471 is a potent, selective, orally available CCR1 antagonist with Ki of 1 nM for hCCR1, displays 100 times less affinity for rat CCR1.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    BX471 hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    BX471 is a potent, selective, orally available CCR1 antagonist with Ki of 1 nM for hCCR1, displays 100 times less affinity for rat CCR1.
  • Description
    BX471 is a potent, selective, orally available CCR1 antagonist with Ki of 1 nM for hCCR1, displays 100 times less affinity for rat CCR1; shows 10,000-fold selectivity for CCR1 compared with 28 GPCRs (); displays CCR1 ligands MIP-1α, RANTES, and MCP-3 with high affinity (Ki=1-5.5 nM), inhibits a number of CCR1-mediated effects including Ca(2+) mobilization, increase in extracellular acidification rate, CD11b expression; effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis.Multiple Sclerosis Discontinued.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    BX-471 hydrochloride | BX 471 hydrochloride
  • Pathway
    GPCR/G Protein
  • Target
    Chemokine Receptor
  • Recptor
    Chemokine Receptor
  • Research Area
    Inflammation/Immunology
  • Indication
    Multiple Sclerosis

Chemical Information

  • CAS Number
    288262-96-4
  • Formula Weight
    471.3526
  • Molecular Formula
    C21H25Cl2FN4O3
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    CC1CN(CCN1C(=O)COC2=C(C=C(C=C2)Cl)NC(=O)N)CC3=CC=C(C=C3)F.Cl
  • Chemical Name
    Urea, N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-, hydrochloride (1:1)

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Horuk R, et al. J Biol Chem. 2001 Feb 9;276(6):4199-204. 2. Anders HJ, et al. J Clin Invest. 2002 Jan;109(2):251-9. 3. Strasly M, et al. Blood. 2004 Jan 1;103(1):40-9. 4. Liang M, et al. J Biol Chem. 2000 Jun 23;275(25):19000-8.
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