2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. 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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TN-783

TN-783 Chemical Structure

CAS No. : 2771021-30-6

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Description

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[1].

IC50 & Target

NLRP3

19.3 nM (IC50)

In Vitro

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.

TN-783 Related Antibodies
In Vivo

TN-783 (0.5-50 mg/kg, p.o., twice daily, 14-66 days) can achieve safe (lean body mass preservation), effective, and reversible weight loss by reducing hypothalamic neuroinflammation[1].

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

Animal Model: Diet-induced obese (DIO) and Normal chow (NC)-fed lean mice[1].
Dosage: 50 mg/kg
Administration: P.o., twice daily for 15 days
Result: Caused a decrease in body weight in DIO mice, but did not affect the body weight of lean mice.
Animal Model: Diet-induced obese (DIO) and Normal chow (NC)-fed lean mice[1].
Dosage: 0.5 mg/kg, 2 mg/kg, 50 mg/kg
Administration: P.o., twice daily for 28 days
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.
Animal Model: Diet-induced obese (DIO) and Normal chow (NC)-fed lean mice[1].
Dosage: 50 mg/kg
Administration: P.o., twice daily for 14-28 days
Result: Reversed microglia activation and significantly alleviated the dysregulation of a large number of genes and protein expression.
Animal Model: Diet-induced obese (DIO) and Normal chow (NC)-fed lean mice[1].
Dosage: 50 mg/kg; Smegglutide: 0.0041 mg/kg (1 nmol/kg)
Administration: P.o., twice daily for 66 days; s.c., once daily for 66 days
Result: Combination therapy produced more significant and sustained weight loss than either drug alone.
Effectively prevented weight rebound.
Molecular Weight

494.18

Formula

C16H11F4IN4O2
CAS No.
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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Purity & Documentation
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TN-783 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TN-7832771021-30-6TN783TN 783NOD-like Receptor (NLR)ObesityNLRP3 inflammasomeHypothalamic inflammationTN-101Inhibitorinhibitorinhibit

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