CAS NO: | 54863-37-5 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
Storage | Store at -20°C |
M.Wt | 133.17 |
Cas No. | 54863-37-5 |
Formula | C4H7NO2S |
Solubility | ≥16.3 mg/mL in DMSO |
Chemical Name | 3-(methylsulfonyl)propanenitrile |
Canonical SMILES | N#CCCS(=O)(C)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Dapansutrile 是有效,选择性和有口服活性的 NLRP3 炎性小体抑制剂。具有抗炎,镇痛活性[1]。在体外,纳摩尔浓度的Dapansutrile能减少典型和非典型NLRP3炎症体激活后IL-1β和IL-18的释放[2]。用Dapansutrile治疗小鼠限制了MSU晶体的关节炎症(p>0.0001),与药物治疗的小鼠相比,滑膜IL-1β、IL-6、骨髓过氧化物酶和CXCL1水平下降(p<0.01)。口服Dapansutrile对改善反应性以及痛风性关节炎非常有效[3]。
参考文献:
[1]. Toldo S, Mauro AG, Cutter Z, Van Tassell BW, Mezzaroma E, Del Buono MG, Prestamburgo A, Potere N, Abbate A. 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. doi: 10.1097/FJC.0000000000000658. PMID: 30747785.
[2]. Marchetti C, Swartzwelter B, Gamboni F, Neff CP, Richter K, Azam T, Carta S, Tengesdal I, Nemkov T, D'Alessandro A, Henry C, Jones GS, Goodrich SA, St Laurent JP, Jones TM, Scribner CL, Barrow RB, Altman RD, Skouras DB, Gattorno M, Grau V, Janciauskiene S, Rubartelli A, Joosten LAB, Dinarello CA. OLT1177, a β-sulfonyl nitrile compound, safe in humans, inhibits the NLRP3 inflammasome and reverses the metabolic cost of inflammation. Proc Natl Acad Sci U S A. 2018 Feb 13;115(7):E1530-E1539. doi: 10.1073/pnas.1716095115. Epub 2018 Jan 29. PMID: 29378952; PMCID: PMC5816172.
[3]. Marchetti C, Swartzwelter B, Koenders MI, Azam T, Tengesdal IW, Powers N, de Graaf DM, Dinarello CA, Joosten LAB. NLRP3 inflammasome inhibitor OLT1177 suppresses joint inflammation in murine models of acute arthritis. Arthritis Res Ther. 2018 Aug 3;20(1):169. doi: 10.1186/s13075-018-1664-2. PMID: 30075804; PMCID: PMC6091035.