Tegaserod maleate - CAS:189188-57-6

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Tegaserod maleate (Synonyms:马来酸替加色罗; SDZ-HTF-919; HTF-919)

目录号 : KM8710 CAS No. : 189188-57-6 纯度 : 98%

Data Sheet SDS 产品使用指南

Tegaserod maleate 是选择性的、5-HT₄ 受体的部分激动剂和 5-HT_2B 受体的拮抗剂。Tegaserod maleate 在胃肠道中表现出促进的作用。

规格	价格	是否有货
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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生物活性

Tegaserod maleate is a selective 5-HT₄ receptor partial agonist and a 5-HT_2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract.

IC₅₀&Target

5-HT₄ Receptor

5-HT_2B Receptor

体外研究

Tegaserod was metabolized in human liver microsomes to O-desmethyl tegaserod at a low rate.
Tegaserod had significant binding affinity for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors (pK_i=7.5, 8.4 and 7.0, respectively).
Tegaserod (0.1-3 μM) inhibits 5-HT-mediated contraction of the rat isolated stomach fundus potently (pA₂=8.3), consistent with 5-HT2B receptor antagonist activity.

体内研究

Tegaserod increases the amplitude of excitatory postsynaptic currents mediated by nicotinic acetylcholine receptors which may contribute to the prokinetic effects by facilitating excitatory neurotransmission in mice.
Tegaserod (0.1 mg/kg) significantly accelerates the gastric emptying rate of glucose in db/db mice, reducing the fraction of the meal remaining in the stomach at 30 min by 80%.
Tegaserod (5, 10, 50, 100 μg/mL) promotes hindlimb motor function at 6 weeks after spinal cord injury compared to the control group receiving vehicle only.

Animal Model:	Female C57BLKS/J db/db mice.
Dosage:	0.1, 0.5, 1.0, 2.0 mg/kg.
Administration:	IP 15 min prior to gastric loading.
Result:	Produced a dramatic decrease in the fraction of the meal remaining in the stomach for doses as low as 0.1 mg/kg (0.1 mg/kg). Accelerated gastric emptying, with a reduction of nearly 80% in the fraction remaining at 30 min (P < 0.0001) (0.1 mg/kg). Induced a significant decrease in the gastric emptying rate as the amount of the meal remaining at 30 min was significantly greater (2.0 mg/kg). Resulted in inhibition of tegaserod-induced increased gastric emptying (0.1 mg/kg).

Animal Model:	Three- to four-month-old female C57BL/6J mice.
Dosage:	5, 10, 50, 100 μg/mL.
Administration:	Alzet pumps into non-injured spinal cords.
Result:	Showed a less intense astrogliosis within and in the vicinity of the compression lesion site when compared to vehicle-only-treated mice. Showed a smaller lesion area when compared to vehicle-onlytreated mice. Showed a higher staining intensity of 5-HT-immunoreactive axons 1 mm rostral, but not caudal to the lesion center as determined in cross-sections and quantification by ImageJ analysis.

分子式

C₂₀H₂₇N₅O₅

分子量

417.46

CAS号

189188-57-6

中文名称

马来酸替加色罗

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

溶解性数据

In Vitro:

DMSO : ≥ 35 mg/mL (83.84 mM)

H₂O : 1 mg/mL (2.40 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3954 mL	11.9772 mL	23.9544 mL
5 mM	0.4791 mL	2.3954 mL	4.7909 mL
10 mM	0.2395 mL	1.1977 mL	2.3954 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。-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: ≥ 2.5 mg/mL (5.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.99 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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% corn oil
Solubility: ≥ 2.5 mg/mL (5.99 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.99 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

临床试验

纯度： 98%

Data Sheet

SDS

产品使用指南

暂无相关参考文献

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器