Acotiamide monohydrochloride trihydrate
目录号 : KM17783 CAS No. : 773092-05-0 纯度 : 98%

Acotiamide monohydrochloride trihydrate 是一种首创的且具有口服活性的胃肠动力药,有潜力用于功能性消化不良的研究。Acotiamide monohydrochloride trihydrate 通过促毒蕈碱受体拮抗作用和乙酰胆碱酯酶 (AChE) 抑制作用增强肠神经元释放的乙酰胆碱,从而增强胃排空和胃部适应性。

规格 价格 是否有货 数量
5mg
In-stock
10mg
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25mg
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50mg
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100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock
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生物活性

Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic receptor antagonism and acetylcholinesterase (AChE) inhibition, thereby enhancing gastric emptying and gastric accommodation.

体外研究

In in vitro studies, Acotiamide inhibits acetylcholine-induced activation of muscarinic M1 and M2 receptors in transformed Xenopus oocytes, with IC50 values of 1.8 and 10.1 μM, respectively. Acotiamide shows no/limited affinity for serotonin 5HT2, 5HT3 or 5HT4 receptors and dopamine D2 receptors.
Acotiamide inhibits AChE activity, inhibits both the slow (competitively) and fast (noncompetitively) inward currents induced by acetylcholine, enhances electrically stimulated contraction of gastric fundus and gastric body, facilitates acetylcholine release from enteric neurons and, using patch-clamp techniques, potentiates L-type voltagedependent Ca current and inhibits GABA-induced current in area postrema neurons.

体内研究

In in vivo animal models, Acotiamide stimulates postprandial gastroduodenal and/or colonic motor activity, and improves delayed but not normal gastric emptying. For example, Acotiamide significantly improves delayed gastric emptying and feeding inhibition in a restraintstress-induced rat model, but does not affect normal gastric emptying or feeding in intact rats.

分子式
C21H37ClN4O8S
分子量
541.06
CAS号
773092-05-0
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL (231.03 mM; Need ultrasonic)

H2O : 3.03 mg/mL (5.60 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 1.8482 mL 9.2411 mL 18.4822 mL
5 mM 0.3696 mL 1.8482 mL 3.6964 mL
10 mM 0.1848 mL 0.9241 mL 1.8482 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 and light)。-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: ≥ 2.08 mg/mL (3.84 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.84 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.84 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.84 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 20.8 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
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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