NLRP3-IN-96
NLRP3-IN-96 is a blood-brain barrier-penetrant NLRP3 inhibitor with a human Kd value of 556 nM. NLRP3-IN-96 inhibits NLRP3 inflammasome activation, suppresses IL-1β release and reduces NLRP3 expression, and inhibits TNF-α production through an NLRP3-independent pathway. NLRP3-IN-96 can be used for research on neuropathic pain.
For research use only. We do not sell to patients.
- CAS No.: 3113161-60-4
- Formula: C23H26ClFN4O2
- Molecular Weight:444.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
NLRP3 556 nM (Kd) |
IL-1β |
TNF-α |
In Vitro
NLRP3-IN-96 (1-10 μM; 24 h) reduces NLRP3 expression in AD-derived hiPSC-microglia stimulated with oAβ or TNFα/IFNγ[1].
NLRP3-IN-96 (1 μM; 24 h) reduces NLRP3 expression in hiPSC-astrocytes after oAβ stimulation[1].
NLRP3-IN-96 (10 μM; 30 min) blocks the binding of [18F]-22 to NLRP3 in wild-type mouse brain slices, supporting its selective binding to NLRP3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AD-derived hiPSC-microglia
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Concentration:1 μM; 10 μM
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Incubation Time:24 h
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Result:oAβ elevated NLRP3 expression; 10 μM NLRP3-IN-96 decreased NLRP3 expression by 2.5-fold.
Did not significantly alter oAβ GFP fluorescent intensity but showed a trending increase in oAβ phagocytosis.
With TNFα/IFNγ stimulation, NLRP3-IN-96 reduced NLRP3 expression, and a lower concentration also comparably suppressed NLRP3 expression.
Microglia morphology changed with longer projections upon NLRP3-IN-96 exposure.
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Cell Line:hiPSC-astrocytes
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Concentration:1 μM
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Incubation Time:24 h
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Result:Decreased NLRP3 expression in hiPSC-astrocytes upon oAβ stimulation.
Parmacokinetics
In Vivo
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:5 mg/kg
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Administration:i.p.; single administration
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Result:Suppressed serum IL-1β.
Plasma TNF-α was decreased.
IL-6 level was not changed.
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Animal Model:C57BL/6 (male)[1]
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Dosage:10 mg/kg and 20 mg/kg
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Administration:i.p.; once daily; beginning on postoperative day 21
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Result:Compound 22 at both 10 mg/kg and 20 mg/kg increased mechanical withdrawal threshold and thermal withdrawal latency.
The 20 mg/kg dose appeared to provide a better analgesic effect.
In CCI mice, compound 22 at 20 mg/kg suppressed hippocampal IL-1β and TNF-α.
Chemical Information
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CAS No. 3113161-60-4
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Molecular Weight 444.93
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Formula C23H26ClFN4O2
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SMILES
CCCOC1=C(CN2N=NC(C(N(C(C)C)CC3=CC=C(F)C=C3)=O)=C2)C=C(Cl)C=C1
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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-96 Related Classifications
HY-189652 Related Classifications
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