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Dapansutrile NLRP3 inhibitor

Name: Dapansutrile
Brand: Selleck Chemicals
SKU: S8907
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8907

Dapansutrile is a novel and selective NLRP3 inflammasome inhibitor.

Chemical Structure

Molecular Weight: 133.17

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S890701 DMSO]100 mg/mL]false]Water]100 mg/mL]false]Ethanol]Insoluble]false Purity: 98%

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Chemical Information, Storage & Stability

Molecular Weight	133.17	Formula	C₄H₇NO₂S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	54863-37-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CS(=O)(=O)CCC#N

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (750.91 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (37.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (37.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	NLRP3 inflammasome ^[1]
In vitro	In vitro, nanomolar concentrations of Dapansutrile reduces IL-1β and IL-18 release following canonical and noncanonical NLRP3 inflammasome activation. In LPS-stimulated human blood-derived macrophages, this compound decreases IL-1β levels by 60% and IL-18 by 70% at concentrations 100-fold lower in vitro than plasma concentrations safely reached in humans. It also reduces IL-1β release and caspase-1 activity in freshly obtained human blood neutrophils.In monocytes isolated from patients with cryopyrin-associated periodic syndrome (CAPS), this chemical inhibits LPS-induced IL-1β release by 84% and 36%. ^[2]
In vivo	Treatment of mice with Dapansutrile limits MSU crystal articular inflammation (p > 0.0001), which is associated with decreased synovial IL-1β, IL-6, myeloperoxidase, and CXCL1 levels (p < 0.01) compared with vehicle-treated mice. Oral administration of this compound is highly effective in ameliorating reactive as well as gouty arthritis.^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/30747785/ [2] https://www.ncbi.nlm.nih.gov/pubmed/?term=29378952 [3] https://www.ncbi.nlm.nih.gov/pubmed/?term=30075804

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06047262	Not yet recruiting	Diabetes Mellitus Type 2	University Hospital Basel Switzerland\|European Union (Horizon Europe Programme)\|State Secretariat for Education Research and Innovation Switzerland\|Olatec Therapeutics LLC	May 2024	Phase 2
NCT05658575	Recruiting	Acute Gout Flare\|Gout Attack\|Gout Flare\|Gouty Arthritis\|Gout\|Arthritis\|Joint Pain	Olatec Therapeutics LLC	January 6 2023	Phase 2\|Phase 3
NCT03595371	Terminated	Schnitzler Syndrome	Olatec Therapeutics LLC\|Radboud University Medical Center	May 15 2018	Phase 2

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