BiochemProbe — Life Science Research Reagents

Rodatristat ethyl free base · Synonyms: KAR5585

Rodatristat ethyl is a first-in-class oral tryptophan hydroxylase 1 Inhibitor.

For research use only. Not for human or veterinary use.

Purity 98+% Stock Inquire

Rodatristat ethyl structure

CAS No.: 1673571-51-1

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
5 mg USD 680.00 BP-01919-5mg In stock Get quote
10 mg USD 980.00 BP-01919-10mg In stock Get quote
25 mg USD 1,780.00 BP-01919-25mg In stock Get quote
50 mg USD 2,780.00 BP-01919-50mg In stock Get quote
100 mg USD 3,780.00 BP-01919-100mg In stock Get quote
500 mg Inquire BP-01919-500mg In stock Inquire
1 g Inquire BP-01919-1g In stock Inquire

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Description

Rodatristat ethyl (KAR5585) is a first-in-class oral 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).

Biological activity

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).

Identifiers

SMILES
ClC1=CC(C2=CC=CC=C2)=C([C@@H](OC3=NC(N)=NC(N4CCC5(CN[C@H](C(OCC)=O)C5)CC4)=C3)C(F)(F)F)C=C1
InChIKey
TZSZZENYCISATO-WIOPSUGQSA-N

Specifications

MW (average)
590.0360
Formula
C29H31ClF3N5O3
CAS No.
1673571-51-1
Physical state
Solid
Color
White to off-white
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -20°C, 1 month

Solubility

Soluble in DMSO : 100 mg/mL

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.

Same research area

Search Cardiovascular Disease