Mosapride citrate dihydrate

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CAS NO:

636582-62-2

TAK-370 citrate dihydrate
AS-4370 citrate dihydrate

Mosapride (TAK-370) citrate dehydrate 是一种胃促动力剂，具有5-羟色胺₄受体（5-hydroxytryptamine₄）激动剂活性，已广泛用于研究多种胃肠道疾病。Mosapride citrate dehydrate 对Kv4.3具有浓度依赖的抑制作用，其IC₅₀值为 15.2 μM。Mosapride citrate dehydrate 在体内实验中也有选择性地刺激上消化道运动。

生物活性

Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with5-hydroxytryptamine₄receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibitsKv4.3in a concentration-dependent manner withIC₅₀values of 15.2 μM^[1]. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo^[2].

IC₅₀& Target

5-HT₄Receptor

Kv4.3

15.2 μM (IC₅₀)

体外研究
(In Vitro)

Mosapride (0.3-30 μM) exhibits an inhibitory activity against Kv4.3 with an IC₅₀of 15.2 μM in a concentration-dependent manner. Mosapride also inhibits the open state of Kv4.3 currents during depolarization and accelerates the closed-state inactivation at subthreshold potentials^[1].

体内研究
(In Vivo)

Mosapride (Intravenous injection;0.3-3 mg/kg) dose-dependently increases the antral motor activity in conscious dogs which indicates that mosapride selectively stimulates upper gastrointestinal motility^[2].

Animal Model:	Beagle dogs^[2]
Dosage:	0.3-3 mg/kg
Administration:	Intravenous injection; 0.3-3 mg/kg
Result:	Increased the antral motor activity dose-dependently in conscious dogs.

Clinical Trial

分子量

650.05

Formula

C₂₇H₃₇ClFN₃O₁₂

CAS 号

636582-62-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.