Dapansutrile

Dapansutrile is a novel and selective NLRP3 inflammasome inhibitor.

Dapansutrile Chemical Structure

Dapansutrile Chemical Structure

CAS: 54863-37-5

Selleck's Dapansutrile has been cited by 1 publication

Purity & Quality Control

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

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Biological Activity

Description Dapansutrile is a novel and selective NLRP3 inflammasome inhibitor.
Targets
NLRP3 inflammasome [1]
In vitro
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, Dapansutrile 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. Dapansutrile 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), Dapansutrile inhibits LPS-induced IL-1β release by 84% and 36%. [2]

In Vivo
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 Dapansutrile is highly effective in ameliorating reactive as well as gouty arthritis.[3]

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
November 2023 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 Unknown status
Schnitzler Syndrome
Olatec Therapeutics LLC|Radboud University Medical Center
May 15 2018 Phase 2

Chemical Information & Solubility

Molecular Weight 133.17 Formula

C4H7NO2S

CAS No. 54863-37-5 SDF --
Smiles CS(=O)(=O)CCC#N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (750.91 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble


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In vivo
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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.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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