1. Immunology/Inflammation
  2. NOD-like Receptor (NLR)
  3. Dapansutrile

Dapansutrile  (Synonyms: OLT1177)

Cat. No.: HY-17629 Purity: ≥98.0%
COA Handling Instructions

Dapansutrile is a potent, orally active and selective NLRP3 inflammasome inhibitor. Dapansutrile has anti-inflammatory activity and decreases immune factor levels. Dapansutrile can be used for research of inflammatory diseases.

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

Dapansutrile Chemical Structure

Dapansutrile Chemical Structure

CAS No. : 54863-37-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 80 In-stock
50 mg USD 280 In-stock
100 mg USD 450 In-stock
200 mg   Get quote  
500 mg   Get quote  

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

Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Dapansutrile is a potent, orally active and selective NLRP3 inflammasome inhibitor. Dapansutrile has anti-inflammatory activity and decreases immune factor levels. Dapansutrile can be used for research of inflammatory diseases[1][2].

IC50 & Target

NLRP3

 

In Vivo

Dapansutrile (3.75 g/kg; p.o.; daily, for 22 d) ameliorates neurological decline and nervous tissue damage in experimental autoimmune encephalomyelitis (EAE) mice[1].
Dapansutrile (3.75 g/kg; p.o.; daily, for 22 d) attenuates the protein levels of pro-inflammatory cytokines in the spinal cord of experimental autoimmune encephalomyelitis (EAE) mice[1].
Dapansutrile (6-600 mg/kg; i.p.; once; male ICR (CD1) mice) reduces infarct size and reduces caspase-1 activity in the heart[2].
Dapansutrile (6-600 mg/kg; i.p.; once, for 24 hours and 7 days; mice subjected to acute myocardial infarction) preserves cardiac function following myocardial ischemia-reperfusion injury[2].

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

Animal Model: EAE-induced female adult C57BL/6 (8–10 weeks old)[1]
Dosage: 3.75 g/kg
Administration: Oral administration; daily, for 22 days
Result: Ameliorated the neurological deficits of EAE disease.
Reduced the levels of IL-1β, L-18 , TNFα, CXCL-1 and IL-6. Showed ~2-fold reduction in the infiltration of T cells (CD45+, CD3+). Reduced the accumulation macrophages (CD45high, CD11b+, F4/80+), microglia (CD45low, CD11b+), and other cells (CD45+, CD11b-, CD3-, CD24+).
Animal Model: Male ICR (CD1) mice (8-12 weeks old)[2]
Dosage: 6, 60, and 600 mg/kg
Administration: Intraperitoneal injection; once
Result: Reduced infarct size in a dose-dependent manner.
Animal Model: Mice subjected to acute myocardial infarction (AMI)[2]
Dosage: 6, 60, and 600 mg/kg
Administration: Intraperitoneal injection; once, for 24 hours and 7 days
Result: Preserved left ventricular (LV) systolic function at 24 hours.
Increased in cardiac function at 7 days of reperfusion when compared with the control mice.
Clinical Trial
Molecular Weight

133.17

Formula

C4H7NO2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CCCS(=O)(C)=O

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 (750.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 36.67 mg/mL (275.36 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 7.5092 mL 37.5460 mL 75.0920 mL
5 mM 1.5018 mL 7.5092 mL 15.0184 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (15.62 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (15.62 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 120 mg/mL (901.10 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: ≥98.0%

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
H2O / DMSO 1 mM 7.5092 mL 37.5460 mL 75.0920 mL 187.7300 mL
5 mM 1.5018 mL 7.5092 mL 15.0184 mL 37.5460 mL
10 mM 0.7509 mL 3.7546 mL 7.5092 mL 18.7730 mL
15 mM 0.5006 mL 2.5031 mL 5.0061 mL 12.5153 mL
20 mM 0.3755 mL 1.8773 mL 3.7546 mL 9.3865 mL
25 mM 0.3004 mL 1.5018 mL 3.0037 mL 7.5092 mL
30 mM 0.2503 mL 1.2515 mL 2.5031 mL 6.2577 mL
40 mM 0.1877 mL 0.9386 mL 1.8773 mL 4.6932 mL
50 mM 0.1502 mL 0.7509 mL 1.5018 mL 3.7546 mL
60 mM 0.1252 mL 0.6258 mL 1.2515 mL 3.1288 mL
80 mM 0.0939 mL 0.4693 mL 0.9386 mL 2.3466 mL
100 mM 0.0751 mL 0.3755 mL 0.7509 mL 1.8773 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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Dapansutrile
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