计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Velusetrag
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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 Parkinson's disease
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 pEC 50 of 8.3. Velusetrag (100 pM-1 μM) produces concentration-dependent contraction of the guinea pig colonic longitudinal muscle/myenteric plexus (LMMP), with a pEC 50 of 7.9. Velusetrag (0.001-10 μM) produces a concentration-dependent relaxation of the carbachol (3 μM)-precontracted rat esophagus, with a pEC 50 of 7.9. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6 mice (7-8 weeks old) were injected with MPTPDosage: 3 mg/kg Administration: A single i.p. Result: Improved facilitation of contextual fear extinction. Did not improve the impaired rotarod performance in PD mice.
IC50& Target:5-HT 4 Receptor 7.7 (pKi)
规格
别名
维鲁斯特拉
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Velusetrag
生化机理
Velusetrag（TD-5108）是一种口服活性、强效和选择性的血清素 5-HT 4 受体（5-HT4R）激动剂，pK i 为 7.7。Velusetrag 对 5-HT 2A 和 5-HT 2B 受体没有亲和力（K i >10 μM）。Velusetrag 可用于研究 5-HT 2A 和 5-HT 2B 受体的 g
储存条件
-80℃储存
运输条件
特低温运输
作用类型
激动剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)N1C2=CC=CC=C2C=C(C1=O)C(=O)NC3C[C@H]4CC[C@@H](C3)N4C[C@H](CN(C)S(=O)(=O)C)O
关联CAS
MeSH Entry Terms
1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid ((1S,3R,5R)-8-((R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl)-8-aza-bicyclo(3.2.1)oct-3-yl)amide;TD-5108;TD5108;velusetrag
分子量
504.64
技术文档
高级数据
产品属性
| ALogP | 1.7 |
|---|
关联靶点（人）
HTR4
Tclin
5-羟色胺受体 4(5-hydroxytryptamine receptor 4)
(0 活性数据)
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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