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 h) displays very low cytotoxicity in HepG2 cells with an IC₅₀ of 16.84 μM^[1].
BNS808 demonstrates a hERG IC₅₀ of 5.39 μM suggesting low potential for cardiotoxicity since its IC₅₀ for CB₁R is 0.8 nM^[1].
BNS808 (0.2 mg/mL, 10 min) exhibits moderate inhibition of CYP3A4, weak-moderate inhibition of CYP2C9 and CYP2C19, and weak inhibition of CYP1A2 and CYP2D6, with IC₅₀ values of 2.99, 8.33, 18.0, and >50 μM, respectively^[1].

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

BNS808 (1 mg/kg, p.o., one single dose) demonstrates limited brain penetrance (an average of 13.7 ng/g) after a single dose at different time points (1-8 h) in C57Bl/6 mice^[1].
BNS808 (1 mg/kg, p.o., 24 d) demonstrates limited brain penetrance (around 20 ng/g) after chronic administration in C57Bl/6 mice^[1].
BNS808 (1-10 mg/kg, p.o.) shows no CNS-mediated side effects in wide-type male C57Bl/6J mice at low (1 mg/kg) and high (10 mg/kg) doses and no significant changes in locomotor activity^[1].
BNS808 (1 mg/kg/day, p.o., 24 days) reduces body weight and improves metabolic profile in diet-induced obese (DIO) C57Bl/6J mice^[1].

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

548.87

C₂₅H₂₀Cl₃N₃O₃S

2836313-12-1

ClC1=CC=C(S(=O)(NC2CCCOC3=C(C4=CC=C(Cl)C=C4)N(C5=C(Cl)C=CC=C5)N=C23)=O)C=C1

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.