NLRP3-IN-12
NLRP3-IN-12 is a specific NLRP3 inflammasome inhibitor. NLRP3-IN-12 reduces the release of IL-1β by targeting the NLRP3 protein, with an IC50 of 0.45 μM. NLRP3-IN-12 can be used for the research of inflammatory bowel disease.
For research use only. We do not sell to patients.
- Formula: C27H32ClNO7
- Molecular Weight:518.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
NLRP3 inflammasome[1]
NLRP3-IN-12 (compound 6E) (0.5-2 μM; pretreated for 1 h) inhibits LPS/ATP-stimulated expression of cleaved caspase-1 and IL-1β in THP-M cells[1].
NLRP3-IN-12 (2 μM) inhibits GSDMD-mediated pyroptosis in THP-M cells[1].
NLRP3-IN-12 (1 μM) exhibits the half-life (T1/2) are 53.4 min and 31.8 min in human and rat liver microsomes, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-M cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:Pretreated for 1 h, then stimulated with LPS (1 μg/mL) for 4.5 h, and ATP (5 mM) for 0.5 h.
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Result:Reduced the secretion of IL-1β and caspase-1.
Had no effect on the levels of NLRP3, pro-IL-1β, ASC, pro-caspase 1, p65, p-p65, IκBα, and p-IκBα.
NLRP3-IN-12 (20 mg/kg; i.v.) exhibits the half-life (T1/2) is 6.64 h, elimination rate constant (Kel) is 0.107 h, clearance rate (CL) is 105 mL/kg/min and steady-state apparent volume of distribution (Vdss) is 23.1 L/kg in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice were induced acute colitis by drinking 3% DSS (dextran sulfate sodium)[1]
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Dosage:5, 10 mg/kg
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Administration:Intraperitoneal injection daily for 10 days in aqueous solution containing DMSO/0.5% CMC-Na/normal saline
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Result:Attenuated DSS-induced weight loss, loose stools, bloody stools, shortened colons, increased disease activity index score, and lower survival rate.
Chemical Information
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Molecular Weight 518.00
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Formula C27H32ClNO7
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SMILES
O[C@@H]1[C@]2(CO3)[C@@]([C@H](O)[C@]3(O)[C@]45[C@@]2([H])CC[C@](C(C5=O)=C)([H])[C@@]4([H])OC(NC6=CC=CC(Cl)=C6)=O)([H])C(C)(C)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NLRP3-IN-12 Related Classifications
HY-151952 Related Classifications
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