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Rodatristat ethyl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rodatristat ethyl图片
CAS NO:1673571-51-1
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品名称
KAR5585
产品介绍
Rodatristat ethyl (KAR5585) 是一种首创的,具有口服活性的tryptophan hydroxylase 1 (TPH1)抑制剂,具有体外纳摩尔浓度,可降低5-hydroxytryptamine (5-HT)的水平并显着降低肺动脉高压 (PAH),
生物活性

Rodatristat ethyl (KAR5585) is a first-in-class oraltryptophan hydroxylase1 (TPH1)Inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of5-HTand significantly reduces pulmonary arterial hypertension (PAH)[1][2].

IC50& Target

5-HT1Receptor

 

TPH1

 

体内研究
(In Vivo)

Rodatristat ethyl (100 or 200 mg/kg; oral administration; once daily; for 28 days; male Sprague-Dawley rats) treatment decreases erum, gut and lung 5-HT levels in a dose-dependent manner and significantly reduces pulmonary arterial pressure, and pulmonary vessel wall thickness and occlusion in male rats with monocrotaline (MCT)[1].

Animal Model:Male Sprague-Dawley rats (175-200 g)[1]
Dosage:100 mg/kg or 200 mg/kg
Administration:Oral administration; once daily; for 28 days
Result:Decreased serum, gut and lung 5-HT levels in a dose-dependent manner and significantly reduced pulmonary arterial pressure, and pulmonary vessel wall thickness and occlusion in male rats.
Clinical Trial
分子量

590.04

Formula

C29H31ClF3N5O3

CAS 号

1673571-51-1

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.