KAR-5585

Modify Date: 2024-01-08 18:57:46

KAR-5585 Structure
KAR-5585 structure
Common Name KAR-5585
CAS Number 1673571-51-1 Molecular Weight 590.04
Density N/A Boiling Point N/A
Molecular Formula C29H31ClF3N5O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of KAR-5585


Rodatristat ethyl (KAR5585) is an orally active tryptophan hydroxylase 1 (TPH1) inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH)[1][2].

 Names

Name Rodatristat ethyl

 KAR-5585 Biological Activity

Description Rodatristat ethyl (KAR5585) is an orally active tryptophan hydroxylase 1 (TPH1) inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH)[1][2].
Related Catalog
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.
References

[1]. Aiello RJ, et al. Tryptophan hydroxylase 1 Inhibition Impacts Pulmonary Vascular Remodeling in Two Rat Modelsof Pulmonary Hypertension. J Pharmacol Exp Ther. 2017 Feb;360(2):267-279.

[2]. Alice Melão, MSc. Early Results on Rodatristat Ethyl Support Launch of Phase 2 Trial in PAH Patients. FEBRUARY 4, 2019.

 Chemical & Physical Properties

Molecular Formula C29H31ClF3N5O3
Molecular Weight 590.04
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