BMS-813160

CAS No. 1286279-29-5

BMS-813160( —— )

Catalog No. M17924 CAS No. 1286279-29-5

BMS-813160 is the first dual?CCR2/CCR5?antagonist to enter Clinical development for cardiovascular.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    BMS-813160
  • Note
    Research use only, not for human use.
  • Brief Description
    BMS-813160 is the first dual?CCR2/CCR5?antagonist to enter Clinical development for cardiovascular.
  • Description
    BMS-813160 is the first dual?CCR2/CCR5?antagonist to enter Clinical development for cardiovascular.(In Vitro):BMS-813160 binds with CCR2, CCR5, CCR1, CCR4 and CXCR2 with IC50s of 6.2 nM, 3.6 nM, >25 μM, >40 μM and >40 μM, respectively.BMS-813160 shows activities to CCR2 CTX, CCR2 CD11b, CCR5 CTX and CCR5 CD11b with IC50s of 0.8, 4.8, 1.1 and 5.7 nM, respectively.(In Vivo):BMS-813160 (10-160 mg/kg; p.o. twice a day for two days) inhibits the migration of inflammatory monocytes and macrophages in mouse thioglycollate-induced peritonitis model, and shows excellent oral bioavailability.
  • In Vitro
    BMS-813160 binds with CCR2, CCR5, CCR1, CCR4 and CXCR2 with IC50s of 6.2 nM, 3.6 nM, >25 μM, >40 μM and >40 μM, respectively.BMS-813160 shows activities to CCR2 CTX, CCR2 CD11b, CCR5 CTX and CCR5 CD11b with IC50s of 0.8, 4.8, 1.1 and 5.7 nM, respectively.
  • In Vivo
    BMS-813160 (10-160 mg/kg; p.o. twice a day for two days) inhibits the migration of inflammatory monocytes and macrophages in mouse thioglycollate-induced peritonitis model, and shows excellent oral bioavailability. Animal Model:Human-CCR2 knock-in C57BL/6 male mice with thioglycollate injectionDosage:10, 50 and 160 mg/kg Administration:Oral gavage; 10-160 mg/kg twice a day; for two days Result:Dose-dependently reduced inflammatory monocyte and macrophage infiltration in the peritoneum.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    Potassium Channel
  • Recptor
    CCR2|CCR5
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1286279-29-5
  • Formula Weight
    484.64
  • Molecular Formula
    C25H40N8O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 25 mg/mL 51.58 mM;
  • SMILES
    CC(C)(C)N[C@@H]1CC[C@@H]([C@H](NC(C)=O)C1)N4CC[C@H](Nc2ncnc3cc(nn23)C(C)(C)C)C4=O
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Norman P. et al. A dual CCR2/CCR5 chemokine antagonist, BMS-813160? Evaluation of WO2011046916. Expert Opin Ther Pat. 2011 Dec;21(12):1919-24.
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