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[CAS NO. 54863-37-5] Dapansutrile
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-17629 |
| Brand: | MCE |
| CAS: | 54863-37-5 |
Overview
| MDL | MFCD11934305 |
|---|---|
| Molecular Weight | 133.17 |
| Molecular Formula | C4H7NO2S |
| SMILES | N#CCCS(=O)(C)=O |
1 Publications Citing Use of MCE
Summary
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
DMSO : ≥ 125 mg/mL ( 938.65 mM )
H 2 O : 36.67 mg/mL ( 275.36 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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 |
-
1.
Add each solvent one by one: PBS
Solubility: 120 mg/mL (901.10 mM); Clear solution; Need ultrasonic
-
2.
-
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
References
- [1] Sánchez-Fernández A, et, al. OLT1177 (Dapansutrile), a Selective NLRP3 Inflammasome Inhibitor, Ameliorates Experimental Autoimmune Encephalomyelitis Pathogenesis. Front Immunol. 2019 Nov 1;10:2578.
- [2] Toldo S, et, al. The NLRP3 Inflammasome Inhibitor, OLT1177 (Dapansutrile), Reduces Infarct Size and Preserves Contractile Function After Ischemia Reperfusion Injury in the Mouse. J Cardiovasc Pharmacol. 2019 Apr;73(4):215-222.
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