[CAS NO. 54863-37-5] Dapansutrile

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PRODUCTS SPECIFICATIONS [54863-37-5]

Catalog

HY-17629

Brand

MCE

CAS

54863-37-5

DESCRIPTION [54863-37-5]

Overview

MDL	MFCD11934305
Molecular Weight	133.17
Molecular Formula	C4H7NO2S
SMILES	N#CCCS(=O)(C)=O

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

1 Publications Citing Use of MCE

[1]Hum Exp Toxicol. 2022 Jan-Dec;41:9603271221145401.

Summary

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] .

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] .

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 (CD45 ^high , CD11b ⁺ , F4/80 ⁺ ), microglia (CD45 ^low , 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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02134964	Olatec Therapeutics LLC	Healthy Volunteers	June 2014	Phase 1
NCT01768975	Olatec Therapeutics LLC	Osteoarthritis of the Knee	January 2013	Phase 2
NCT04971499	April Salama, M.D.\|Merck Sharp & Dohme LLC\|Olatec Therapeutics LLC\|Duke University	Melanoma	September 6, 2022	Phase 1\|Phase 2
NCT01636141	Olatec Therapeutics LLC	Healthy Volunteers	June 2012	Phase 1
NCT03534297	Olatec Therapeutics LLC	Systolic Heart Failure	May 16, 2018	Phase 1
NCT04540120	Olatec Therapeutics LLC\|CTI Clinical Trial and Consulting Services	Covid19\|Cytokine Release Syndrome	September 25, 2020	Phase 2
NCT03595371	Olatec Therapeutics LLC\|Radboud University Medical Center	Schnitzler Syndrome	May 15, 2018	Phase 2
NCT02104050	Olatec Therapeutics LLC	Osteoarthritis\|Pain	April 2014	Phase 2

Appearance

Solid

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 ( 938.65 mM )

H ₂ O : 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
10 mM	0.7509 mL	3.7546 mL	7.5092 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 120 mg/mL (901.10 mM); Clear solution; Need ultrasonic
2.

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
3.

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
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (15.62 mM); Clear solution

* All of the co-solvents are available by MCE.