Velusetrag (TD-5108) hydrochloride 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 hydrochloride 对 5-HT2A和 5-HT2B受体没有亲和力 (Ki>10 μM)。Velusetrag hydrochloride 可用于胃肠道疾病和帕金森病的研究。
生物活性 | Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin5-HT4receptor(5-HT4R), with apKiof 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2Aand 5-HT2Breceptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease[1][2][3][4][5]. |
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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 pEC50of 8.3[1]. Velusetrag (100 pM-1 μM) produces concentration-dependent contraction of the guinea pig colonic longitudinal muscle/myenteric plexus (LMMP), with a pEC50of 7.9[1]. TD-5108 (0.001-10 μM) produces a concentration-dependent relaxation of the carbachol (3 μM)-precontracted rat esophagus, with a pEC50of 7.9[1].
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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[3]. Velusetrag (3 mg/kg; a single i.p.) increase hippocampal cAMP levels in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated mice[3]. 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[2]. Velusetrag (0.003-1 mg/kg; a single i.v.) dose-dependently increases inter-crystal distance, consistent with relaxation of the oesophagus in rats[2].
Animal Model: | Male C57BL/6 mice (7-8 weeks old) were injected with MPTP[3] | Dosage: | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 220 mg/mL(406.58 mM;Need ultrasonic) H2O : 10 mg/mL(18.48 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 1.8481 mL | 9.2404 mL | 18.4809 mL | 5 mM | 0.3696 mL | 1.8481 mL | 3.6962 mL | 10 mM | 0.1848 mL | 0.9240 mL | 1.8481 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 5.5 mg/mL (10.16 mM); Clear solution
此方案可获得 ≥ 5.5 mg/mL (10.16 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 5.5 mg/mL (10.16 mM); Clear solution
此方案可获得 ≥ 5.5 mg/mL (10.16 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 5.5 mg/mL (10.16 mM); Clear solution
此方案可获得 ≥ 5.5 mg/mL (10.16 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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