Velusetrag hydrochloride TD-5108 hydrochloride|cas:866933-51-9|西域试剂

Velusetrag hydrochloride TD-5108 hydrochloride,96.65%

产品编号：Bellancom-10457A| CAS NO：866933-51-9| 分子式：C₂₅H₃₇ClN₄O₅S| 分子量：541.10

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货号	价格	库存与货期
Bellancom-10457A	￥3500.00	杭州北京（现货）
Bellancom-10457A	￥5800.00	杭州北京（现货）
Bellancom-10457A	￥11000.00	杭州北京（现货）
Bellancom-10457A	￥17000.00	杭州北京（现货）

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Velusetrag hydrochloride TD-5108 hydrochloride

产品介绍

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，pK_i 为 7.7。Velusetrag hydrochloride 对 5-HT_2A 和 5-HT_2B 受体没有亲和力 (K_i>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 serotonin 5-HT₄ receptor (5-HT₄R), with a pK_i of 7.7. Velusetrag hydrochloride exhibits no affinity (K_i>10 μM) for 5-HT_2A and 5-HT_2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease^[4]^[5].

体外研究

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.
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.

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

体内研究

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.) increase 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.

西域 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
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.

体内研究

西域 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
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.

性状

Solid

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。