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产品总数：61429
| 商品编号 | 规格 | 价格 | 会员价 | 是否有货 | 数量 |
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| PL01497-5mg | 5mg | ¥5625.00 | 请登录 |
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| PL01497-10mg | 10mg | ¥9322.00 | 请登录 |
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| PL01497-25mg | 25mg | ¥17680.00 | 请登录 |
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| PL01497-50mg | 50mg | 询价 | 询价 |
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| PL01497-100mg | 100mg | 询价 | 询价 |
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| PL01497-10mM*1mLinDMSO | 10mM*1mLinDMSO | ¥6188.00 | 请登录 |
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| 中文名称 |
Velusetrag
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|---|---|
| 中文别名 |
1,2-二氢-N-[(3-内)-8-[(2R)-2-羟基-3-[甲基(甲磺酰基)氨基]丙基]-8-氮杂双环[3.2.1]辛-3-基]-1-(1-甲基乙基)-2-氧代-3-喹啉甲酰胺
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| 英文名称 |
Velusetrag
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| 英文别名 |
1,2-Dihydro-N-[(3-endo)-8-[(2R)-2-hydroxy-3-[methyl(methylsulfonyl)amino]propyl]-8-azabicyclo[3.2.1]oct-3-yl]-1-(1-methylethyl)-2-oxo-3-quinolinecarboxamide;3-QUINOLINECARBOXAMIDE, 1,2-DIHYDRO-N-[(3-ENDO)-8-[(2R)-2-HYDROXY-3-[METHYL(METHYLSULFONYL)AMINO]PROPYL]-8-AZABICYCLO[3...;N-[8-[(2R)-2-hydroxy-3-[methyl(methylsulfonyl)amino]propyl]-8-azabicyclo[3.2.1]octan-3-yl]-2-oxo-1-propan-2-ylquinoline-3-carboxamide;TD 5108(Velusetrag)
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| Cas No. |
866933-46-2
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| 分子式 |
C25H36N4O5S
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| 分子量 |
504.64
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| 包装储存 |
Powder -20°C 3 years；4°C 2 years
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| 详情描述 |
Velusetrag (TD-5108) 是一种具有口服活性，有效和选择性的血清素 5-HT4 受体 (5-HT4R) 激动剂，pKi 为 7.7。Velusetrag 对 5-HT2A 和 5-HT2B 受体没有亲和力 (Ki>10 μM)。Velusetrag 可用于胃肠道疾病和帕金森病的研究。
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| 产品详情 |
Velusetrag (TD-5108) 是一种具有口服活性，有效和选择性的血清素 5-HT4 受体 (5-HT4R) 激动剂，pKi 为 7.7。Velusetrag 对 5-HT2A 和 5-HT2B 受体没有亲和力 (Ki>10 μM)。Velusetrag 可用于胃肠道疾病和帕金森病的研究。
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|---|---|
| 生物活性 |
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT 4 receptor (5-HT4R), with a pK i of 7.7. Velusetrag exhibits no affinity (K i >10 μM) for 5-HT 2A and 5-HT 2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinsons disease.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
5-HT4 Receptor 7.7 (pKi)
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| 体外研究(In Vitro) |
Velusetrag (10 pM-100 μM) concentration-dependently increases the cAMP in HEK-293 cells stably transfected with the h5-HT4(c) receptor, with a pEC50 of 8.3.Velusetrag (100 pM-1 μM) produces concentration-dependent contraction of the guinea pig colonic longitudinal muscle/myenteric plexus (LMMP), with a pEC50 of 7.9.Velusetrag (0.001-10 μM) produces a concentration-dependent relaxation of the carbachol (3 μM)-precontracted rat esophagus, with a pEC50 of 7.9. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
Velusetrag (3 mg/kg; a single i.p.) significantly improves the facilitation of contextual fear extinction in PD mice.
Velusetrag (3 mg/kg; a single i.p.) increases hippocampal cAMP levels in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated mice.
Velusetrag (0.003-3 mg/kg; a single s.c.) increases colonic transit in a dose-dependent manner and reduces the time taken for excretion of the dye in guinea pigs.
Velusetrag (0.003-1 mg/kg; a single i.v.) dose-dependently increases inter-crystal distance, consistent with relaxation of the oesophagus in rats. 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]. Smith JAM, et, al. The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):125-37.[2]. Beattie DT, et, al. The in vivo gastrointestinal activity of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):139-47.
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| 溶解度数据 |
In Vitro: DMSO : 100 mg/mL (198.16 mM; Need ultrasonic)配制储备液
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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。
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