Dapansutrile
(Synonyms: 3-methanesulfonyl Propanenitrile) 目录号 : GC34555
Dapansutrile是一种口服小分子选择性NLRP3炎症小体抑制剂。
Cas No.:54863-37-5
Sample solution is provided at 25 µL, 10mM.
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Dapansutrile is an oral, small-molecule, selective NLRP3 inflammasome inhibitor [1]. Dapansutrile blocks the assembly and activation of NLRP3, Dapansutrile inhibits downstream caspase-1 activation and the maturation and release of IL-1β and IL-18, alleviating the inflammatory response [2-3]. Dapansutrile is primarily used to treat gouty arthritis [4].
In chondrocytes, Low-dose Dapansutrile (0-10μM; 24h) had no significant cytotoxicity to rat chondrocytes [5]. In BV2 cells, Dapansutrile (100μM; 24h) inhibits cell proliferation [6].
In db/db mouse model, Dapansutrile (200mg/kg; ip; 8 weeks) treatment can alleviate dyslipidemia and hepatic lipid metabolism and function [7]. In acute myocardial infarction mouse model, Dapansutrile (6-600mg/kg; ip; single injection) treatment reduced infarct size in a dose-dependent manner [8].
References:
[1]. Sánchez-Fernández A, Skouras D B, Dinarello C A, et al. OLT1177 (Dapansutrile), a selective NLRP3 inflammasome inhibitor, ameliorates experimental autoimmune encephalomyelitis pathogenesis[J]. Frontiers in immunology, 2019, 10: 2578.
[2]. Toldo S, Mauro A G, Cutter Z, et al. The NLRP3 inflammasome inhibitor, OLT1177 (dapansutrile), reduces infarct size and preserves contractile function after ischemia reperfusion injury in the mouse[J]. Journal of Cardiovascular Pharmacology, 2019, 73(4): 215-222.
[3]. Elsayed M S, Abu-Elsaad N M, Nader M A. The NLRP3 inhibitor dapansutrile attenuates folic acid induced nephrotoxicity via inhibiting inflammasome/caspase-1/IL axis and regulating autophagy/proliferation[J]. Life sciences, 2021, 285: 119974.
[4]. Klück V, Tim L, Janssen M, et al. Dapansutrile, an oral selective NLRP3 inflammasome inhibitor, for treatment of gout flares: an open-label, dose-adaptive, proof-of-concept, phase 2a trial[J]. The Lancet Rheumatology, 2020, 2(5): e270-e280.
[5]. Tang L, Sim I, Moqbel S A A, et al. Dapansutrile ameliorated chondrocyte inflammation and osteoarthritis through suppression of MAPK signaling pathway[J]. Human & Experimental Toxicology, 2022, 41: 09603271221145401.
[6]. Wu P, Tang X, Cui K, et al. OLT1177 (Dapansutrile) Attenuates Retinal Neovascularization by Inhibiting NLRP3 Inflammasome Activation[J]. Investigative Ophthalmology & Visual Science, 2022, 63(7): 1759–F0219-1759–F0219.
[7]. Wu Y, Zhou J. Dapansutrile Regulates Mitochondrial Oxidative Stress and Reduces Hepatic Lipid Accumulation in Diabetic Mice[J]. Current Issues in Molecular Biology, 2025, 47(3): 148.
[8]. Toldo S, Mauro A G, Cutter Z, et al. The NLRP3 inflammasome inhibitor, OLT1177 (dapansutrile), reduces infarct size and preserves contractile function after ischemia reperfusion injury in the mouse[J]. Journal of Cardiovascular Pharmacology, 2019, 73(4): 215-222.
Dapansutrile是一种口服小分子选择性NLRP3炎症小体抑制剂 [1]。Dapansutrile阻断NLRP3的组装和激活，抑制下游caspase-1的活化以及IL-1β和IL-18的成熟和释放，从而减轻炎症反应 [2-3]。Dapansutrile主要用于治疗痛风性关节炎 [4]。
在软骨细胞中，低剂量Dapansutrile（0-10μM；24h）对大鼠软骨细胞无显著细胞毒性 [5]。在BV2细胞中，Dapansutrile（100μM；24h）可抑制细胞增殖 [6]。
在db/db小鼠模型中，Dapansutrile（200mg/kg；ip；8周）治疗可改善血脂异常、肝脏脂质代谢和功能 [7]。在急性心肌梗死小鼠模型中，Dapansutrile（6-600mg/kg；ip；单次注射）治疗以剂量依赖性方式减少梗死面积 [8]。
| Cell experiment [1]: | |
Cell lines | Chondrocytes |
Preparation Method | Chondrocytes (5 × 103 cells/well) were seeded into 96-well plates, and then treated with different concentrations of Dapansutrile (0, 1, 2, 5, and 10μM) for 24h. The medium was replaced with fresh medium containing 10% CCK-8 solution, and then the cells were incubated at 37℃ for 3h. Optical density (OD) was determined at a wavelength of 450nm. |
Reaction Conditions | 0-10μM; 24h |
Applications | Low-dose Dapanshulide had no significant cytotoxicity to rat chondrocytes. |
| Animal experiment [2]: | |
Animal models | db/db mouse model |
Preparation Method | Using a db/db mouse model whose fasting blood glucose levels were measured ≥ 11.1mM twice (approximately 12h apart). The model mice were divided into two groups: the model group (treated with an intraperitoneal injection of physiological saline) and the Dapansutrile group, which received a daily intraperitoneal injection of Dapansutrile at a dose of 200mg/kg (dissolved in physiological saline) |
Dosage form | 200mg/kg; ip; 8 weeks |
Applications | Dapansutrile treatment can alleviate dyslipidemia and hepatic lipid metabolism and function in db/db. |
References: | |
| Cas No. | 54863-37-5 | SDF | |
| 别名 | 3-methanesulfonyl Propanenitrile | ||
| Canonical SMILES | N#CCCS(=O)(C)=O | ||
| 分子式 | C4H7NO2S | 分子量 | 133.17 |
| 溶解度 | DMSO : ≥ 125 mg/mL (938.65 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 7.5092 mL | 37.546 mL | 75.092 mL |
| 5 mM | 1.5018 mL | 7.5092 mL | 15.0184 mL |
| 10 mM | 0.7509 mL | 3.7546 mL | 7.5092 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet