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。
| 生物活性 | Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin5-HT4receptor(5-HT4R), with apKiof 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2Aand 5-HT2Breceptors. Velusetrag 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].
Velusetrag (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.) increases 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 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(198.16 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9816 mL | 9.9081 mL | 19.8161 mL | | 5 mM | 0.3963 mL | 1.9816 mL | 3.9632 mL | | 10 mM | 0.1982 mL | 0.9908 mL | 1.9816 mL |
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以下溶剂前显示的百
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此方案可获得 ≥ 5.75 mg/mL (11.39 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 57.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 5.48 mg/mL (10.86 mM); Clear solution
此方案可获得 ≥ 5.48 mg/mL (10.86 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 54.8 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。 *以上所有助溶剂都可在本网站选购。
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