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Cat. No.: HY-190915

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NLRP3-IN-103

NLRP3-IN-103 is an orally active, selective NLRP3 inhibitor with a K_d value of 120.7 nM for hNLRP3. NLRP3-IN-103 does not affect NLRC4- or AIM2-mediated IL-1β release, nor does it affect NF-κB-dependent TNF-α and IL-6 production. NLRP3-IN-103 blocks NLRP3-dependent Pyroptosis. NLRP3-IN-103 can be used for research on ulcerative colitis.

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Formule: C₂₇H₁₈N₄OS
Masse moléculaire:446.52

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

NLRP3-IN-103 Chemical Structure

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Quantité

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]

NLRP3 inflammasome

120.7 nM (Kd)

Voir tous les produits spécifiques à Isoform NOD-like Receptor (NLR) :

Cellular Effect

Cell Line	Type	Value	Description	References
J774.A1	IC50	0.16 μM	Inhibition of LPS/ATP-induced IL-1β release in murine J774A.1 macrophages assessed by ELISA after 0.5 h L22 pre-incubation and 0.5 h ATP stimulation. Inhibition of LPS/ATP-induced IL-1β release in murine J774A.1 macrophages assessed by ELISA after 0.5 h L22 pre-incubation and 0.5 h ATP stimulation.	42911702
J774.A1	CC₅₀	>100 μM	Cytotoxicity against murine J774A.1 macrophages assessed after 24 h incubation with L22 showing CC₅₀ greater than 100 μM. Cytotoxicity against murine J774A.1 macrophages assessed after 24 h incubation with L22 showing CC₅₀ greater than 100 μM.	42911702

In Vitro

InflammasomeInnate ImmunityCytokines and ChemokinesPyroptosisOthers

Inflammasome

NLRP3-IN-103 (78.125-20000 nM) directly binds the NLRP3 NACHT domain with a K_D of 357.8 nM (full-length NLRP3 K_D = 120.7 nM) and does not bind the PYD domain^[1].

Innate Immunity

Cytokines and Chemokines

NLRP3-IN-103 (0.4-10 μM; 1 h) does not inhibit NF-κB-driven TNF-α or IL-6 production in J774A.1 macrophages up to 10 μM^[1].

Innate Immunity

Inflammasome

NLRP3-IN-103 (Compound L22) (0.04-30 μM; 0.5 h) potently inhibits NLRP3 inflammasome-mediated IL-1β release in J774A.1 macrophages, with an IC₅₀ of 0.16 μM^[1].
NLRP3-IN-103 (10 μM; 1 h) is a selective NLRP3 inflammasome inhibitor in J774A.1 macrophages and shows no activity against NLRC4 or AIM2 inflammasomes at 10 μM^[1].
NLRP3-IN-103 (1-10 μM) inhibits NLRP3 inflammasome activation (caspase-1 p20 and mature IL-1β) in J774A.1 and U937 macrophages, but not the NF-κB priming step^[1].

Innate Immunity

Inflammasome

Pyroptosis

NLRP3-IN-103 (0.1-30 μM; 0.5 h) dose-dependently inhibits NLRP3-dependent pyroptosis (LDH release) in THP-1 macrophages^[1].

Others

NLRP3-IN-103 (24 h) shows low cytotoxicity in J774A.1, AML-12, and HL-7702 cells, with CC₅₀ values above 100 μM^[1].
NLRP3-IN-103 (up to 48 h) is stable in gastrointestinal fluid, dog and rat plasma, and rat liver homogenate^[1].

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

ELISA Assay^[1]

Cell Line:

J774A.1 murine macrophages
Concentration:

0.04, 0.1, 0.4, 1.1, 3.3, 10, 30 μM (0.5 h pre-incubation; 0.5 h ATP stimulation); 1 μM and 10 μM (inhibition-rate determination)
Incubation Time:

0.5 h pre-incubation; 0.5 h ATP stimulation
Result:

Dose-dependently suppressed LPS/ATP-induced IL-1β secretion.
Inhibition rates were 69.4% at 1 μM and 82.1% at 10 μM.
IC₅₀ = 0.16 μM, approximately 10-fold more potent than istradefylline (IC₅₀ = 1.81 μM).

ELISA Assay^[1]

Cell Line:

J774A.1 macrophages
Concentration:

0.4, 1.1, 3.3, 10 μM (1 h pre-exposure; 6 h LPS stimulation)
Incubation Time:

1 h pre-exposure; 6 h LPS stimulation
Result:

Did not significantly inhibit LPS-induced IL-6 or TNF-α production across 0.4-10 μM, indicating independence from NF-κB suppression.

Parmacokinetics

Species	Dose	Route	AUC_0-∞	T_1/2	Clearance (CL)	T_max	C_max	V_ss	F
Mice^[1]	2.5 mg/kg	i.v.	6421.06 ng·h/mL	4.26 h	400.24 mL/h/kg	0.08 h	8070.43 ng/mL	744.71 mL/kg	/
Mice^[1]	20 mg/kg	p.o.	13017.36 ng·h/mL	7.49 h	/	2.67 h	1300.18 ng/mL	/	22.94 %

In Vivo

InflammasomeCytokines & Chemokines

Inflammasome

Cytokines & Chemokines

NLRP3-IN-103 (20-40 mg/kg; p.o.; single dose; 1 h before LPS) reduces NLRP3-driven IL-1β levels in LPS-challenged C57BL/6 mice without reducing TNF-α^[1].
NLRP3-IN-103 (20-40 mg/kg; p.o.; once daily; from day 1 through day 8) ameliorates DSS-induced colitis in C57BL/6J mice, reducing disease activity, colon shortening, and colonic NLRP3 inflammasome activation^[1].

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

Animal Model:

C57BL/6 (male, 6-8 weeks, 25-30 g)^[1]
Dosage:

20 mg/kg; 40 mg/kg
Administration:

p.o.; single dose; 1 h before LPS
Result:

Reduced IL-1β levels at 20 mg/kg and 40 mg/kg.
TNF-α remained unaffected.

Animal Model:

C57BL/6J (male, 6-8 weeks)^[1]
Dosage:

20 mg/kg; 40 mg/kg
Administration:

p.o.; once daily; from day 1 through day 8
Result:

Ameliorated body-weight loss at 20 mg/kg and 40 mg/kg, lowered DAI scores, and reversed colon shortening.
Colonic IL-1β and caspase-1 p20 levels were suppressed, and histology showed epithelial regeneration with reduced inflammatory cell infiltration.

Related Protocols :

Chemical Information

Masse moléculaire 446.52
Formule C₂₇H₁₈N₄OS
SMILES

N#CC1=CC=C(CN(C=NC2=C3C(CN4C5=C(C6=C4C=CC=C6)C=CC=C5)=CS2)C3=O)C=C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Jiang Y, et al. Design, Synthesis, and Anti-Inflammatory Activity Evaluation of Novel thieno[2,3-d]Pyrimidin-4(3H)-One-Based NLRP3 Inflammasome Inhibitors. J Med Chem. 2026 Oct 22;69(20):24657-24681. [Content Brief]

Calculators

Calculateur de molarité

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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NLRP3-IN-103

Voir tous les produits spécifiques à Isoform NOD-like Receptor (NLR)

Activité biologique

Description

IC50 & Target

Cellular Effect

In Vitro

Parmacokinetics

In Vivo

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

NLRP3-IN-103 Related Classifications

HY-190915 Related Classifications

Bioz

Keywords

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