KAR-5585

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KAR-5585 (Rodatristat) 是强效 TPH1 抑制剂 KAR5417 的前药。

KAR-5585 (Rodatristat) is the prodrug of the potent TPH1 inhibitor KAR5417, shows robust reduction of intestinal serotonin (5-HT) levels in mice; generates high and sustained systemic exposure of the active parent KAR5417 in rats and dogs; orally bioavailable.Hypertension Phase 1 Clinical.

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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 ratswith monocrotaline (MCT). Animal Model:Male Sprague-Dawley rats (175-200 g)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.

KAR5585 | Rodatristat

Metabolic Enzyme/Protease

TPH

TPH

Cardiovascular Disease

Hypertension

1673571-51-1

590.044

C29H31ClF3N5O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (169.48 mM)

O=C([C@H]1NCC2(CCN(C3=NC(N)=NC(O[C@H](C4=CC=C(Cl)C=C4C5=CC=CC=C5)C(F)(F)F)=C3)CC2)C1)OCC

ethyl (S)-8-(2-amino-6-((R)-1-(5-chloro-[1,1'-biphenyl]-2-yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-3-carboxylate

(-20℃)

With Ice Pack

≥ 2 years