| Identification | Back Directory | [Name]
NT-0796 | [CAS]
2272917-13-0 | [Synonyms]
NT-0796
2-Pyrimidinepropanoic acid, α-[[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl)amino]carbonyl]oxy]-, 1-methylethyl ester, (αR)- | [Molecular Formula]
C23H27N3O4 | [MOL File]
2272917-13-0.mol | [Molecular Weight]
409.48 |
| Chemical Properties | Back Directory | [Boiling point ]
526.8±50.0 °C(predicted) | [density ]
1.275±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [solubility ]
Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml | [form ]
Solid | [pka]
12.96±0.20(predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
NT-0796 is an inhibitor of the NOD-like receptor protein 3 (NLRP3) inflammasome and a prodrug form of NDT-19795.1 It selectively inhibits NLRP3 over NLR family CARD domain-containing protein 4 (NLRC4) at 3 nM, as well as a panel of 121 other receptors at 10 µM, but does inhibit the serotonin (5-HT) receptor subtype 5-HT2B by 90% at 10 µM. NT-0796 inhibits LPS- and ATP-induced IL-1β release in isolated human peripheral blood mononuclear cells (PBMCs) and whole blood (IC50s = 0.32 and 6.8 nM, respectively), however, it does not affect LPS-induced TNF-α or IL-6 release in isolated human PBMCs (IC50s = >2 µM for both), indicating NLRP3 selectivity. It decreases body weight, food intake, and plasma levels of total cholesterol, HDL, and proprotein convertase subtilisin kexin type 9 (PCSK9) in a model of high-fat diet-induced obesity using transgenic mice expressing human carboxylesterase-1 (CES1), the enzyme that converts NT-0796 to NDT-19795, when administered at a dose of 100 mg/kg three times per day.2WARNING This product is not for human or veterinary use. | [References]
[1] DAVID HARRISON. Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders.[J]. Journal of Medicinal Chemistry, 2023: 14897-14911. DOI: 10.1021/acs.jmedchem.3c01398
[2] PETER THORNTON. Reversal of High Fat Diet-Induced Obesity, Systemic Inflammation, and Astrogliosis by the NLRP3 Inflammasome Inhibitors NT-0249 and NT-0796.[J]. Journal of Pharmacology and Experimental Therapeutics, 2024: 813-826. DOI: 10.1124/jpet.123.002013 |
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nanjing
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www.linye-e.com/ |
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