BMS-813160

SKU: orb1222775

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.

Key Properties

• CAS Number: 1286279-29-5
• MW: 484.64
• Purity: >98% (HPLC)
• Formula: C₂₅H₄₀N₈O₂
• 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
• Target: Potassium Channel
• Solubility: DMSO : 25 mg/mL 51.58 mM

Bioactivity

• 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 injection. Dosage: 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Potassium Channel