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
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
ETA
Available Sizes
Frequently Asked Questions
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