TA-0201

TA-0201 is a novel orally active, competitive, non-peptide endothelin receptor antagonist. TA-0201 antagonizes the specific binding of [125I]ET-1 to cloned human receptors of ETA and ETB with Ki values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1[1].

Product Specifications

CAS Number

[169679-53-2]

UNSPSC

12352005

Target

Endothelin Receptor

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Smiles

O=S(NC1=NC=NC(OCCOC2=NC=C(C=N2)Br)=C1C3=CC=C(C)C=C3)(C4=CC=C(C(C)(CO)C)C=C4)=O

Molecular Formula

C27H28BrN5O5S

Molecular Weight

614.51

References & Citations

[1]Ohashi N, et al. Determination of TA-0201, a novel orally active non-peptide endothelin antagonist, in rat plasma and tissues by a liquid chromatography--electrospray ionization--tandem mass spectrometry system. J Pharm Biomed Anal. 1999 Mar;19 (3-4) :491-9.