| 中文名称 |
Dapansutrile
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| 中文别名 |
3-甲磺酰基丙腈;3-(甲基磺酰基)丙腈
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| 英文名称 |
Dapansutrile
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| 英文别名 |
Propanenitrile, 3-(methylsulfonyl)-;3-(Methylsulfonyl)propanenitrile;Dapansutrile;3-methanesulfonylpropanenitrile;OLT1177;3-methylsulfonylpropanenitrile;3-(methanesulfonyl)propanenitrile;2Z03364G96;Dapansutrile [INN];Dapansutrile(OLT1177);Dapansutrile (USAN/INN);Dapansutrile [USAN:INN];Dapansutrile (OLT1177);3-Methylsulfonylpropionitrile;3-methylsulphonyl-propionitrile;GTPL10056;BDBM50505850;s8907
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| Cas No. |
54863-37-5
|
| 分子式 |
C4H7NO2S
|
| 分子量 |
133.17
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
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| 详情描述 |
Dapansutrile 是一种口服有效的选择性 NLRP3 炎症小体抑制剂。Dapansutrile 具有抗炎活性,能够降低免疫因子水平。Dapansutrile 可用于炎性疾病的研究。
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| 产品详情 |
Dapansutrile 是一种口服有效的选择性 NLRP3 炎症小体抑制剂。Dapansutrile 具有抗炎活性,能够降低免疫因子水平。Dapansutrile 可用于炎性疾病的研究。
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| 生物活性 |
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.
|
| 性状 |
Solid
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| 体内研究(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.
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.
Dapansutrile (6-600 mg/kg; i.p.; once; male ICR (CD1) mice) reduces infarct size and reduces caspase-1 activity in the heart.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years;4°C 2 years
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| ClinicalTrial |
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| 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.[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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| 溶解度数据 |
In Vitro: DMSO : ≥ 125 mg/mL (938.65 mM)H2O : 36.67 mg/mL (275.36 mM; Need ultrasonic)
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[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.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。