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.
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- CAS No.: 2836313-12-1
- Formule: C25H20Cl3N3O3S
- Masse moléculaire:548.87
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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CYP2C9 2.99 μM (IC50) |
CYP2C19 8.33 μM (IC50) |
CYP1A2 18.0 μM (IC50) |
CYP2D6 >50 μM (IC50) |
CB1R 0.8 nM (IC50) |
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., 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.
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Animal Model:Diet-induced obese (DIO) male C57Bl/6J mice [1]
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Dosage:1 mg/kg/day, 24 days
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Administration:Oral gavage (p.o.)
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Result:Reduced body weight attributing to a reduction in total body fat with a significant increase in lean body mass.
Suggested a trend toward substantial effects of the drug on glucose homeostasis and reduced glucose levels in fasting conditions.
Demonstrated efficacy in reversing hepatic steatosis and hepatocellular damage.
Led to a significant reduction in liver triglyceride content and liver enzymes, including ALT, AST, and ALP.
Chemical Information
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CAS No. 2836313-12-1
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Masse moléculaire 548.87
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Formule C25H20Cl3N3O3S
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SMILES
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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BNS808 Related Classifications
HY-172808 Related Classifications
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