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    Neuronal Signaling
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  3. Velusetrag hydrochloride

Velusetrag hydrochloride (Synonyms: TD-5108 hydrochloride)

目录号: HY-10457A 纯度: 96.65%
产品使用指南

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。

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Velusetrag hydrochloride Chemical Structure

Velusetrag hydrochloride Chemical Structure

CAS No. : 866933-51-9

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease[1][2][3][4][5].

IC50 & Target[1]

5-HT4 Receptor

7.7 (pKi)

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[1].
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[1].
TD-5108 (0.001-10 μM) produces a concentration-dependent relaxation of the carbachol (3 μM)-precontracted rat esophagus, with a pEC50 of 7.9[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

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 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.
Clinical Trial
分子量

541.10

Formula

C25H37ClN4O5S

CAS 号
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°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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 MCE 网站选购。
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
Velusetrag hydrochloride
目录号:
HY-10457A
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