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CXCR2-IN-1

CAS No. 1873376-49-8

CXCR2-IN-1( —— )

Catalog No. M12902 CAS No. 1873376-49-8

A potent, CNS penetrant CXCR2 antagonist with pIC50 of 9.3; shows neutrophil chemotaxis inhibition with pIC50 of 7.6.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    CXCR2-IN-1
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, CNS penetrant CXCR2 antagonist with pIC50 of 9.3; shows neutrophil chemotaxis inhibition with pIC50 of 7.6.
  • Description
    A potent, CNS penetrant CXCR2 antagonist with pIC50 of 9.3; shows neutrophil chemotaxis inhibition with pIC50 of 7.6; has developability profiles (CYP inhibition pIC<5.0, and hERG binding affinity pIC<4.0); exhibits favorable PK profile, reasonable CNS penetration, and good developability potential; orally bioavailable.
  • In Vitro
    CXCR2 plays an important role in the activation and recruitment of neutrophils to sites of inflammation. CXCR2-IN-1 (compound 22) shows favorable central nervous system penetration property (Br/Bl>0.45).
  • In Vivo
    CXCR2-IN-1 shows efficacy in a cuprizone-induced demyelination model through oral administration, providing evidence to support CXCR2 to be a potential therapeutic target to treat demyelinating diseases such as multiple sclerosis.
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    Chemokine Receptor
  • Recptor
    Chemokine Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1873376-49-8
  • Formula Weight
    476.3492032
  • Molecular Formula
    C19H20Cl2FN3O4S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥5.4 mg/mL (Need ultrasonic and warming)
  • SMILES
    CN1CCC(CC1)S(=O)(=O)C2=C(C=CC(=C2O)NC(=O)NC3=C(C(=CC=C3)F)Cl)Cl
  • Chemical Name
    Urea, N-(2-chloro-3-fluorophenyl)-N'-[4-chloro-2-hydroxy-3-[(1-methyl-4-piperidinyl)sulfonyl]phenyl]-

Shipping & Storage Information

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

Reference

1. Xu H, et al. ACS Med Chem Lett. 2016 Feb 8;7(4):397-402.
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