2. Immunology/Inflammation
  3. NOD-like Receptor (NLR) Interleukin Related
  4. NLRP3-IN-42

NLRP3-IN-42 (compound H28) is a potent NLRP3 inhibitor with an KD value of 1.15 µM. NLRP3-IN-42 decreases the LPS (HY-D1056) induced protein expression of cleaved-caspase-1 (p20). NLRP3-IN-42 selectively inhibits IL-1β release.

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NLRP3-IN-42 Chemical Structure

NLRP3-IN-42 Chemical Structure

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NLRP3-IN-42 Related Antibodies

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Description

NLRP3-IN-42 (compound H28) is a potent NLRP3 inhibitor with an KD value of 1.15 µM. NLRP3-IN-42 decreases the LPS (HY-D1056) induced protein expression of cleaved-caspase-1 (p20). NLRP3-IN-42 selectively inhibits IL-1β release[1].

IC50 & Target[1]

NLRP3

1.15 μM (Kd)

IL-1β

 

In Vitro

NLRP3-IN-42 (compound H28) (0-30 µM) decreases the LPS (HY-D1056) induced protein expression of cleaved-caspase-1 (p20) in a dose-dependent manner[1].
NLRP3-IN-42 can stably bind to the ADP active site of the NLRP3 NACHT domain[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NLRP3-IN-42 Related Antibodies

Western Blot Analysis[1]

Cell Line: J774A.1 cells
Concentration: 0, 3, 10, 30 µM
Incubation Time: 2.5 h + 30 min
Result: Decreased the LPS (1 μg/mL) induced protein expression of cleaved-caspase-1 (p20) in culture supernatants (SN) and whole cell lysates (WCL) in a dose-dependent manner.
In Vivo

NLRP3-IN-42 (10 mg/kg; i.p.) selectively inhibits IL-1β release by inhibiting the NLRP3 inflammasome without significantly affecting the inflammatory factor TNF-α[1].
Pharmacokinetic Parameters (ICR mice)[1].

PK parameters H28
Administered dose (mg/kg) iv at 2.5 mg/kg
AUC0-∞ (h*ng/mL) 1189 ± 137
t1/2 (h) 1.69 ± 0.38
CL (mL/h/kg) 35.36 ± 4.12
Cmax (ng/mL) 2987 ± 281

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4-8 weeks, Male C57BL/6 mice[1]
Dosage: 10 mg/kg
Administration: I.p; 1 h before injection of LPS (35 mg/kg, ip) for 2.5 h
Result: Significantly inhibited IL-1β production in the treatment mice. It is noteworthy that the treatment with these compounds do not result in significant inhibition of TNF-α levels.
Molecular Weight

572.66

Formula

C29H27F3N2O3S2
SMILES

CCCNS(=O)(C1=CC=C(C2=CC=CC=C2N(CC3=CC=C(C(F)(F)F)C=C3)C(CC4=CSC=C4)=O)C=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NLRP3-IN-42 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NLRP3-IN-42NOD-like Receptor (NLR)Interleukin RelatedILcleaved-caspase-1 (p20)J774A.1 cellsIL-1βLPSTNF-αInhibitorinhibitorinhibit

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