Darusentan

Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors[1]. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM[2].

Product Specifications

CAS Number

[171714-84-4]

Product Name Alternative

Lu-135252

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Endothelin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/darusentan.html

Purity

98.67

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

COC1=NC(O[C@H](C(O)=O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)=NC(OC)=C1

Molecular Formula

C22H22N2O6

Molecular Weight

410.42

Precautions

H302, H315, H319, H335

References & Citations

[1]Liang F, et al. Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries. Can J Physiol Pharmacol. 2010 Aug;88 (8) :840-9.|[2]Frank Enseleit, et al. Darusentan, a selective endothelin A receptor antagonist, for the oral treatment of resistant hypertension. Ther Adv Cardiovasc Dis. 2010 Aug;4 (4) :231-40.|[3]H H Dao, et al. Norepinephrine-induced aortic hyperplasia and extracellular matrix deposition are endothelin-dependent. J Hypertens. 2001 Nov;19 (11) :1965-73.