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

NLRP3-IN-2, an intermediate substrate in the synthesis of glyburide, inhibits the formation of the NLRP3 inflammasome in cardiomyocytes and limits the infarct size following myocardial ischemia/reperfusion in the mouse, without affecting glucose metabolism.

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NLRP3-IN-2 Chemical Structure

NLRP3-IN-2 Chemical Structure

CAS No. : 16673-34-0

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Based on 1 publication(s) in Google Scholar

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Description

NLRP3-IN-2, an intermediate substrate in the synthesis of glyburide, inhibits the formation of the NLRP3 inflammasome in cardiomyocytes and limits the infarct size following myocardial ischemia/reperfusion in the mouse, without affecting glucose metabolism[1].

IC50 & Target

NLRP3

 

In Vivo

NLRP3-IN-2 is well tolerated with no effects on the glucose levels in vivo[1].
NLRP3-IN-2 (100 mg/kg) treatment in a model of AMI due to ischemia+reperfusion significantly inhibits the activity of inflammasome (caspase-1) in the heart by 90% (P<0.01) and reduced infarct size, measured at pathology (by >40%, P<0.01) and with troponin I levels (by >70%, P<0.01) [1].

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

Animal Model: Experimental acute myocardial infarction (AMI) model in mice[1].
Dosage: 100 mg/kg.
Administration: Intraperitoneal administration 30 minutes prior to surgery, then every 6 hours for 3 additional doses.
Result: Led to a significant >90% reduction in caspase-1 activity (reflective of the formation of an active inflammasome) in the heart tissue measured 24 hours after ischemia.
Led to a significant reduction in the infarct size measured with TTC (>40% reduction) or troponin I levels (>70% reduction) when compared with vehicle alone.
Molecular Weight

368.84

Formula

C16H17ClN2O4S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NCCC1=CC=C(S(=O)(N)=O)C=C1)C2=CC(Cl)=CC=C2OC
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 : 125 mg/mL (338.90 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 2.7112 mL 13.5560 mL 27.1120 mL
5 mM 0.5422 mL 2.7112 mL 5.4224 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.

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  • Dilution Calculator

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (5.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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

Purity: ≥98.0%

SDS (393 KB)

COA (246 KB) HNMR (213 KB)

Handling Instructions (2659 KB)
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 2.7112 mL 13.5560 mL 27.1120 mL 67.7801 mL
5 mM 0.5422 mL 2.7112 mL 5.4224 mL 13.5560 mL
10 mM 0.2711 mL 1.3556 mL 2.7112 mL 6.7780 mL
15 mM 0.1807 mL 0.9037 mL 1.8075 mL 4.5187 mL
20 mM 0.1356 mL 0.6778 mL 1.3556 mL 3.3890 mL
25 mM 0.1084 mL 0.5422 mL 1.0845 mL 2.7112 mL
30 mM 0.0904 mL 0.4519 mL 0.9037 mL 2.2593 mL
40 mM 0.0678 mL 0.3389 mL 0.6778 mL 1.6945 mL
50 mM 0.0542 mL 0.2711 mL 0.5422 mL 1.3556 mL
60 mM 0.0452 mL 0.2259 mL 0.4519 mL 1.1297 mL
80 mM 0.0339 mL 0.1695 mL 0.3389 mL 0.8473 mL
100 mM 0.0271 mL 0.1356 mL 0.2711 mL 0.6778 mL
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NLRP3-IN-2 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:

NLRP3-IN-216673-34-0NOD-like Receptor (NLR)ischemiareperfusioninflammasomeacutemyocardialinfarctionInhibitorinhibitorinhibit

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