NLRP3-IN-104
NLRP3-IN-104 is a NLRP3 inhibitor that inhibits NLRP3 inflammasome activation. NLRP3-IN-104 reduces pyroptosis and IL-1β release, and inhibits hERG potassium channel activity. NLRP3-IN-104 shows selectivity in the CEREP target panel. NLRP3-IN-104 can be used for research on inflammation-related diseases.
For research use only. We do not sell to patients.
- CAS No.: 3021546-64-2
- Formula: C20H25N5
- Molecular Weight:335.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
NLRP3 |
IL-1β |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
5 nM
|
Inhibition of NLRP3-dependent pyroptosis in human THP-1 monocytic cells.
Inhibition of NLRP3-dependent pyroptosis in human THP-1 monocytic cells.
|
acsmedchemlett.6c00422?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as |
In Vitro
The free fraction of NLRP3-IN-104 in human plasma is 29%, and the free fraction in mouse plasma is 9.7%[1].
The mouse P-gp Papp of NLRP3-IN-104 is 230 nm/s, with an efflux ratio of 7.4[1].
NLRP3-IN-104 inhibits hERG with an IC20 of 1.2 µM, and exhibits an IC20 >10 µM against CaV1.2 and NaV1.5[1].
NLRP3-IN-104 shows good selectivity in the CEREP panel, with five non-kinase hit targets showing 56-80% inhibition at 10 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
Chemical Information
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CAS No. 3021546-64-2
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Molecular Weight 335.45
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Formula C20H25N5
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SMILES
CC1=C(C2=CC=C(N=N2)N[C@H]3CN(CCC3)CC)C=C4C(C=CN4)=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)