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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
Tropisetron
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
89565-68-4
- 规格:
5mg/10mg/25mg/50mg/100mg
| 规格: | 5mg | 产品价格: | ¥302.0 |
|---|---|---|---|
| 规格: | 10mg | 产品价格: | ¥490.0 |
| 规格: | 25mg | 产品价格: | ¥700.0 |
| 规格: | 50mg | 产品价格: | ¥1090.0 |
| 规格: | 100mg | 产品价格: | ¥1790.0 |
| 基本信息 | |
| CAS | No.89565-68-4 |
| 中文名称 | 托烷司琼 |
| 英文名称 | Tropisetron |
| 别名 | ICS 205-930;Tropisetronum;SDZ-ICS-930 free base |
| 分子式 | C17H20N2O2 |
| 分子量 | 284.35 |
| 溶解性 | Soluble in Water/DMSO(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| MDL | MFCD00864399 |
| SMILES | CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 |
| InChIKey | ZNRGQMMCGHDTEI-FUNVUKJBSA-N |
| InChI | InChI=1S/C17H20N2O2/c1-19-11-6-7-12(19)9-13(8-11)21-17(20)15-10-18-16-5-3-2-4-14(15)16/h2-5,10-13,18H,6-9H2,1H3/t11-,12+,13 |
| PubChem CID | 656665 |
| 靶点 | 5-HT Receptor;nAChR |
| 通路 | Neuronal Signaling;GPCR & G Protein;Membrane Transporter&Ion Channel |
| 背景说明 | 是5-HT3受体拮抗剂,也是α7-CHN2受体激动剂。 |
| 生物活性 | Tropisetron 是一种α7CHN2受体激动剂,同时也是5-羟色胺(5-HT)3 受体拮抗剂,IC50为70.1 nM,具有镇痛和抗炎活性。[1] |
| IC50 | 5-HT3 Receptor:70.1μM(IC50)[1] |
| In Vitro | Tropisetron specifically inhibited both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Tropisetron inhibited both the binding to DNA and the transcriptional activity of NFAT and AP-1. Tropisetron is a potent inhibitor of PMA plus ionomycin-induced NF-(kappa)B activation.[2] The anti-inflammatory effects of the 5-HT receptor antagonist tropisetron,are mediated by a selective inhibition of pro-inflammatory cytokines at the post-transcriptional level. Tropisetron prevents the phosphorylation and thus activation of the p38 MAPK.[3] |
| 细胞实验 | Tropisetron failed to reduce cerebral infarction. Animals receiving tropisetron showed a significant increase(p < 0.05)in neurological deficits and mortality rate. Blockade of 5-HT3 receptors with tropisetron worsens ischemic brain injury induced by pMCAO.[4] |
| 动物实验 | Two different doses of tropisetron(5 and 10 mg/kg)or vehicle were administered intraperitoneally 30 min before pMCAO. Neurological deficit scores,mortality rate and infarct volume were determined 24 h after permanent focal cerebral ischemia.[4] |
| 数据来源文献 | [1]. Macor JE,et al. The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist. Bioorg Med Chem Lett. 2001 Feb 12;11(3):319-21. [2]. Vega Lde L,et al. The 5-HT3 receptor antagonist tropisetron inhibits T cell activation by targeting the calcineurin pathway. Biochem Pharmacol. 2005 Aug 1;70(3):369-80. [3]. Stratz C,et al. The anti-inflammatory effects of the 5-HT receptor antagonist tropisetron are mediated by the inhibition of p38 MAPK activation in primary human monocytes. Int Immunopharmacol. 2012 Aug;13(4):398-402. [4]. Candelario-Jalil E,et al. Detrimental effects of tropisetron on permanent ischemic stroke in the rat. BMC Neurosci. 2008 Feb 6;9:19. doi: 10.1186/1471-2202-9-19. |
| 单位 | 瓶 |
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