2. Immunology/Inflammation Apoptosis
  3. NOD-like Receptor (NLR) Pyroptosis
  4. JT002

JT002 is an orally active and selective NLRP3 inflammasome assembly inhibitor. JT002 reduces NLRP3-dependent proinflammatory cytokine (such as IL-1β, IL-1α, IL-18) production and pyroptosis. JT002 blocks NLRP3 inflammasome complex formation. JT002 reduces airway hyperresponsiveness and airway neutrophilia in mice. JT002 can be used for the study of a variety of inflammatory diseases, such as Muckle-Wells syndrome (MWS).

For research use only. We do not sell to patients.

JT002

JT002 Chemical Structure

CAS No. : 2238820-43-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

JT002 Related Antibodies

Top Publications Citing Use of Products

View All NOD-like Receptor (NLR) Isoform Specific Products:

View All Isoforms
NLRP3 NLRP1 NOD1 NOD2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JT002 is an orally active and selective NLRP3 inflammasome assembly inhibitor. JT002 reduces NLRP3-dependent proinflammatory cytokine (such as IL-1β, IL-1α, IL-18) production and pyroptosis. JT002 blocks NLRP3 inflammasome complex formation. JT002 reduces airway hyperresponsiveness and airway neutrophilia in mice. JT002 can be used for the study of a variety of inflammatory diseases, such as Muckle-Wells syndrome (MWS)[1].

In Vitro

In human peripheral blood mononuclear cells (hPBMCs) treated with Lipopolysaccharides (HY-D1056) (LPS) and activated with ATP (HY-B2176), JT002 shows concentration-dependent inhibition of IL-1α, IL-1β and IL-18 production with mean IC50 values of 3 nM, 4 nM and 4 nM, respectively, with no effect on TNFα production[1].
Under LPS plus Nigericin (HY-127019) stimulating conditions, JT002 inhibits IL-1β production from human, mouse and rat PBMCs with mean IC50 values of 6, 25 and 159 nM, respectively[1].
In human and mouse blood stimulated with LPS plus ATP, JT002 shows concentration-dependent inhibition of IL-1β production with mean IC50 values of 100 nM and 94 nM, respectively[1].
JT002 inhibits pyroptosis in LPS plus nigericin stimulated mouse bone-marrow derived macrophages (mBMDMs) as measured by cellular ATP content, with a mean IC50 value of 7 nM[1].
JT002 blocks canonical NLRP3-dependent IL-1β production activated downstream of ATP, Nigericin, cholesterol crystals (CHC) or monosodium urate (MSU) with mean IC50 values of 5 nM, 23 nM, 2 nM and 3 nM, respectively and inhibits non-canonical induced IL-1β production with a mean IC50 value of 30 nM[1].
JT002 shows no inhibition of IL-1β production after NLRP1, NLRC4 or AIM2 activation at concentrations up to 10 µM[1].
JT002 blocks NLRP3 inflammasome complex formation and downstream pathway activation. JT002 inhibits cellular caspase-1 activity with an IC50 of 8 nM in human PBMCs[1].

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

JT002 Related Antibodies
Parmacokinetics
Species Dose Route Plasma Concentration T1/2 AUC Clearance (CL) Vd Tmax Bioavailability
Dog[1] 1 mg/kg i.v. 7.0 μg/mL 1.1 h 10.6 μg·h/mL 1.8 mL/min/kg 0.2 L/kg / /
Dog[1] 1 mg/kg p.o. 4.0 μg/mL 1.4 h 11.6 μg·h/mL / / 1.0 h 100 %
Rat[1] 1 mg/kg i.v. 10.6 μg/mL 2.8 h 16.2 μg·h/mL 1.0 mL/min/kg 0.2 L/kg - h - %
Rat[1] 5 mg/kg p.o. 15.6 μg/mL 23.4 h 59.2 μg·h/mL - mL/min/kg / 0.5 h 73.2 %
In Vivo

JT002 (30 mg/kg; oral gavage; once daily; 30 days) in the Nlrp3A350V/+CreT knock-in mice (mimicking human Muckle-Wells syndrome) prevents body weight loss, reduces liver inflammation and fibrosis, decreases liver alanine aminotransferase levels, and normalizes circulating white blood cell and neutrophil counts[1].
JT002 (2.5-25 mg/kg; oral gavage; once daily; from Day 23-29) in ovalbumin (OVA)-sensitized, OVA-challenged, and induced regulatory T cell (iTreg)-transferred CD8a-/- mice (mimicking IL-17-dependent neutrophilic asthma). The 25 mg/kg dose of JT002 significantly reduces airway hyperresponsiveness and airway neutrophilia, decreases submucosal inflammatory cell infiltration, reduces the concentrations of IL-6 and IL-17 in bronchoalveolar lavage fluid, and increases the INFγ concentration. The 2.5 mg/kg dose of JT002 has no significant effect[1].
JT002 (2.5 mg/kg and 25 mg/kg; oral gavage; once daily; 4 days) in female C57BL6/J mice (a model of ozone - induced neutrophilic asthma). The 25 mg/kg dose of JT002 prevents ozone-induced airway hyperresponsiveness, significantly reduces the number of neutrophils in bronchoalveolar lavage fluid, and reduces airway epithelial desquamation. The 2.5 mg/kg dose of JT002 has no significant effect[1].

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

Animal Model: Nlrp3A350V/+CreT knock-in mice (male and female, 6-8 weeks ol)[1].
Dosage: 30 mg/kg
Administration: Oral gavage, once daily, for 30 days starting on Day 1
Result: Prevented body weight loss.
Significantly reduced the liver weight as a percentage of body weight.
Serum levels of alanine aminotransferase were decreased.
Hepatic expression of pro-inflammatory and profibrotic genes was downregulated.
Animal Model: CD8a-/- C57BL6/j female mice (6-8 weeks old). The mice were sensitized by intraperitoneal injection of 20 μg OVA emulsified in 2.25 mg alum hydroxide on Days 0 and 14, and then received aerosol challenges with 1% OVA in PBS for 20 min each day on three consecutive days (Days 26-28)[1].
Dosage: 2.5 mg/kg and 25 mg/kg
Administration: Oral gavage, once daily, from Day 23-29
Result: The high dose significantly decreased airway hyperresponsiveness and airway neutrophilia, visibly decreased submucosal inflammatory cell infiltration, decreased the concentrations of BAL IL-6 and IL-17, and increased BAL INFγ concentrations.
Animal Model: Female C57BL6/J mice (8-12 weeks old). Mice were exposed to 1.0 ppm of O3 for 3 h[1].
Dosage: 2.5 mg/kg and 25 mg/kg
Administration: Oral gavage, once daily, for 4 days
Result: The high dose prevented ozone-induced airway hyperresponsiveness, significantly reduced BAL fluid neutrophil numbers, and visibly reduced the appearance of epithelial cells in the airway lumen
Clinical Trial
Molecular Weight

432.49

Formula

C20H24N4O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NS(=O)(C1=C(OC[C@@H](OC)C2)N2N=C1)=O)NC3=C(CCC4)C4=CC5=C3CCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (231.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3122 mL 11.5610 mL 23.1219 mL
5 mM 0.4624 mL 2.3122 mL 4.6244 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3122 mL 11.5610 mL 23.1219 mL 57.8048 mL
5 mM 0.4624 mL 2.3122 mL 4.6244 mL 11.5610 mL
10 mM 0.2312 mL 1.1561 mL 2.3122 mL 5.7805 mL
15 mM 0.1541 mL 0.7707 mL 1.5415 mL 3.8537 mL
20 mM 0.1156 mL 0.5780 mL 1.1561 mL 2.8902 mL
25 mM 0.0925 mL 0.4624 mL 0.9249 mL 2.3122 mL
30 mM 0.0771 mL 0.3854 mL 0.7707 mL 1.9268 mL
40 mM 0.0578 mL 0.2890 mL 0.5780 mL 1.4451 mL
50 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1561 mL
60 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9634 mL
80 mM 0.0289 mL 0.1445 mL 0.2890 mL 0.7226 mL
100 mM 0.0231 mL 0.1156 mL 0.2312 mL 0.5780 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

JT002 Related Classifications

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:

JT0022238820-43-2JT 002JT-002NOD-like Receptor (NLR)Pyroptosisinflammationairway hyperresponsivenessneutrophiliaIL-1βIL-1αIL-18NLRP3 inflammasomeInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
JT002
Cat. No.:
HY-149478
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (254 KB) Français - FR (254 KB) Deutsch - DE (254 KB) Norwegian - NO (254 KB) Español - ES (254 KB) Swedish - SV (254 KB) Italian - IT (254 KB) Korean - KR (254 KB) Portuguese - PT (254 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.