TN-783
TN-783 is an orally active, brain-penetrant NLRP3 (IC50 = 19.3 nM) inhibitor. TN-783 enhances the effects of the GLP-1 receptor agonist semaglutide. TN-783 requires sustained targeted action, not permanent metabolic remodeling. TN-783 can be used for the study of obesity.
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- Fòrmula: C16H11F4IN4O2
- Peso molecular:494.18
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
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NLRP3 19.3 nM (IC50) |
TN-783 (2 h) can effectively inhibit the secretion of IL-1β (IC50 = 45.9 nM) by THP-1 cells, under Lipopolysaccharides (HY-D1056) (LPS)/Nigericin (HY-127019) stimulation[1].
TN-783 (0.3 nM-6 μM, 1 h) can dose-dependently inhibit the secretion of IL-1β (IC50 = 5.17 nM) and IL-18 (IC50 = 12.3 nM) in THP-1 cells induced by Palmitic acid (HY-N0830)-BSA complex[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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) and Normal chow (NC)-fed lean mice[1].
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Dosage:50 mg/kg
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Administration:P.o., twice daily for 15 days
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Result:Caused a decrease in body weight in DIO mice, but did not affect the body weight of lean mice.
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Animal Model:Diet-induced obese (DIO) and Normal chow (NC)-fed lean mice[1].
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Dosage:0.5 mg/kg, 2 mg/kg, 50 mg/kg
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Administration:P.o., twice daily for 28 days
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Result:50 mg/kg induced progressive and sustained weight loss in DIO mice; lower doses were ineffective.
The weight loss was due to a significant reduction in fat mass, while lean body mass was preserved. It did not affect lean mice.
The weight loss was driven by sustained inhibition of food intake, without altering weight-corrected energy expenditure or activity levels.
Improved glucose tolerance in DIO mice.
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Animal Model:Diet-induced obese (DIO) and Normal chow (NC)-fed lean mice[1].
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Dosage:50 mg/kg
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Administration:P.o., twice daily for 14-28 days
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Result:Reversed microglia activation and significantly alleviated the dysregulation of a large number of genes and protein expression.
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Animal Model:Diet-induced obese (DIO) and Normal chow (NC)-fed lean mice[1].
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Dosage:50 mg/kg; Smegglutide: 0.0041 mg/kg (1 nmol/kg)
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Administration:P.o., twice daily for 66 days; s.c., once daily for 66 days
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Result:Combination therapy produced more significant and sustained weight loss than either drug alone.
Effectively prevented weight rebound.
Chemical Information
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Peso molecular 494.18
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Fòrmula C16H11F4IN4O2
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SMILES
O=C(NC1=NC=C(C=N1)F)CN2C[C@H](C3=C(C2=O)C=CC(I)=C3)C(F)(F)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TN-783 Related Classifications
HY-179131 Related Classifications
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