BNS808 

BNS808 is an orally active and selective cannabinoid-1 receptor (CB₁R) antagonist (IC₅₀ = 0.8 nM) with notable CB₂R selectivity and minimal brain penetration. BNS808 is studied in research on obesity and its associated metabolic complications, such as metabolic dysfunctional-associated steatotic liver disease (MASLD). BNS808 has reduced free drug availability for CNS entry, enhancing safety and minimizing drug-drug interactions through high plasma binding^[1].

BNS808 (72 小时) 在 HepG2 细胞中表现出极低的细胞毒性，IC₅₀ = 16.84 μM^[1]。
BNS808 的 hERG IC₅₀ = 5.39 μM，表明其对 CB₁R 的 IC₅₀ 为 0.8 nM，具有较低的心脏毒性潜力^[1]。
BNS808 (0.2 mg/mL, 10 分钟) 对 CYP3A4 表现出中度抑制，对 CYP2C9 和 CYP2C19 表现出弱中度抑制，对 CYP1A2 和 CYP2D6 表现出弱抑制，IC₅₀ 值分别为 2.99、8.33、18.0 和 >50 μM。分别为^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

BNS808 (1 mg/kg，口服，单次给药) 在 C57Bl/6 小鼠中不同时间点 (1-8小时) 单次给药后，脑渗透性有限 (平均13.7 ng/g)^[1]。
BNS808 (1 mg/kg，口服，24天) 在 C57Bl/6 小鼠中长期给药后，脑渗透性有限 (约20 ng/g)^[1]。
BNS808 (1-10 mg/kg，口服) 在低剂量 (1 mg/kg) 和高剂量 (10 mg/kg) 野生雄性 C57Bl/6J 小鼠中均未发现中枢神经系统介导的副作用，且运动活动无显著变化^[1]。
BNS808 (1 mg/kg/天，口服，24 天) 可减轻饮食诱导的肥胖 (DIO) C57Bl/6J 小鼠的体重并改善代谢状况^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

548.87

C₂₅H₂₀Cl₃N₃O₃S

2836313-12-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Gammal A, et al., Synthesis and Pharmacological Characterization of Novel Peripheral Cannabinoid-1 Receptor Blockers Based on a Tricyclic Scaffold. J Med Chem. 2025 Apr 21.  [Content Brief]