NLRP3-IN-102
NLRP3-IN-102 is an NLRP3 inhibitor that binds the NACHT domain and blocks inflammasome activation. NLRP3-IN-102 has Kd values of 0.73 μM and 1.41 μM for the human target. NLRP3-IN-102 binds LC3 and NLRP3. NLRP3-IN-102 reduces IL-1β levels in an acute colitis model without reducing NLRP3 protein levels. NLRP3-IN-102 can be used for research on inflammatory bowel disease.
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- Fòrmula: C19H18ClN3O
- Peso molecular:339.82
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
NLRP3 0.73-1.41 μM (Kd) |
LC3 2.54 μM (Kd) |
IL-1β |
In Vitro
NLRP3-IN-102 loses most of its IL-1β inhibitory activity after washout in THP-1 macrophages, with IC50 increasing from 1.05 μM to 43.50 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NLRP3-IN-102 (20 mg/kg; intraperitoneal injection; once daily; 10 days of dosing followed by 7 days off) cannot maintain NLRP3 depletion or durable anti-inflammatory efficacy in DSS colitis after cessation of administration[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[1]
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Dosage:20 mg/kg
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Administration:i.p.; once daily; 10 consecutive days
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Result:Attenuated DSS-induced body-weight loss and DAI elevation, mitigated colon shortening, and reduced colonic IL-1β by ELISA.
Western blot showed that mature IL-1β was lowered without reducing NLRP3 protein levels.
Immunohistochemistry showed diminished colonic IL-1β signal but not NLRP3 signal.
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Animal Model:C57BL/6[1]
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Dosage:20 mg/kg
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Administration:i.p.; once daily; 10-day administration phase followed by 7 days without drug
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Result:After the 7-day drug-free period, mice showed residual DAI above control, body weight below control, and colon length shorter than control.
IL-1β suppression was less durable after withdrawal, and NLRP3 protein remained elevated.
H&E staining showed incomplete mucosal healing and residual inflammatory infiltration after washout.
Chemical Information
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Peso molecular 339.82
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Fòrmula C19H18ClN3O
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SMILES
ClC1=CC=C(C2=C(C)C=C(N[C@@H](C)C3=CC=CC=C3)N=N2)C(O)=C1
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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
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NLRP3-IN-102 Related Classifications
HY-190872 Related Classifications
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