Dapansutrile
Based on 5 publication(s) in Google Scholar
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.92%
- CAS 番号: 54863-37-5
- 分子式: C4H7NO2S
- 分子量:133.17
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Dapansutrile
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ELISA
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
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WB
生物活性
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NLRP3 |
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.
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Animal Model:EAE-induced female adult C57BL/6 (8–10 weeks old)[1]
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Dosage:3.75 g/kg
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Administration:Oral administration; daily, for 22 days
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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+).
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Animal Model:Male ICR (CD1) mice (8-12 weeks old)[2]
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Dosage:6, 60, and 600 mg/kg
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Administration:Intraperitoneal injection; once
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Result:Reduced infarct size in a dose-dependent manner.
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Animal Model:Mice subjected to acute myocardial infarction (AMI)[2]
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Dosage:6, 60, and 600 mg/kg
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Administration:Intraperitoneal injection; once, for 24 hours and 7 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 54863-37-5
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性状 Solid
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分子量 133.17
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分子式 C4H7NO2S
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Color White to off-white
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SMILES
N#CCCS(=O)(C)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Int J Mol Med
Remimazolam alleviates myocardial ischemia/reperfusion injury and inflammation via inhibition of the NLRP3/IL‑1β pathway in mice. [Abstract]2025 Apr;55(4):57. PMID: 39886966
Dapansutrile purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2025 Apr;55(4):57. [Abstract]
Dapansutrile (DAPA: 5 μM) inhibited the LPS-induced release of IL-1β, IL-6 and TNF-α in Raw264.7 cells, while treatment with Rema did not affect the alterations induced by DAPA.
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J Inflamm Res
NLRP3 Mediates NOXs-Induced Iron Overload and Inflammation but Not Oxidative Damage in Colons of DSS-Treated Mice. [Abstract]2025 Apr 4:18:4695-4708. PMID: 40201574
Dapansutrile purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2025 Apr 4:18:4695-4708. [Abstract]
DPI and Dapansutrile (0.00001mg/kg) significantly ameliorated weight loss caused by DSS.
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J Microbiol Immunol Infect
Potential role of intratumoral Fusobacterium nucleatum and interleukin-1 beta in breast cancer cell growth. [Abstract]2025 Jun 7:S1684-1182(25)00119-7. PMID: 40506319
Dapansutrile purchased from MedChemExpress. Usage Cited in: J Microbiol Immunol Infect. 2025 Jun 7:S1684-1182(25)00119-7. [Abstract]
Representative images of a clonogenic assay of cells infected with F. nucleatum 34597 and treated with 10 μM Dapansutrile.
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Hum Exp Toxicol
Dapansutrile ameliorated chondrocyte inflammation and osteoarthritis through suppression of MAPK signaling pathway. [Abstract]2022 Jan-Dec:41:9603271221145401. PMID: 36508695 -
Sci Total Environ
NLRP3 inflammasome activation triggers severe inflammatory liver injury in N, N-dimethylformamide-exposed mice. [Abstract]2024 Jun 15:929:172653. PMID: 38649053
Dapansutrile purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2024 Jun 15:929:172653. [Abstract]
NLRP3 inhibitors ameliorate acute DMF-induced inflammatory liver injury. Mice were treated with MCC950 (25 mg/kg bw) or Dapansutrile (60 mg/kg bw) before and 12 h after DMF exposure (2.0 g/kg bw).H&E staining.
Dapansutrile purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2024 Jun 15:929:172653. [Abstract]
NLRP3 inhibitors ameliorate acute DMF-induced inflammatory liver injury. Mice were treated with MCC950 (25 mg/kg bw) or Dapansutrile (60 mg/kg bw) before and 12 h after DMF exposure (2.0 g/kg bw).Representative western blot bands of NLRP3, caspase-1, cleaved-IL-1β, ASC, GSDMD and GAPDH.
溶剤 & 溶解度
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
Add each solvent one by one: PBS
Solubility: 120 mg/mL (901.10 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (279 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
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.
Dapansutrile 関連分類
HY-17629 関連分類
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