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Darusentan

CAT: 0804-HY-15404-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-15404-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
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

Alternative Products

CatalogName
BA5315-50Darusentan
A21280-5Darusentan 5mg
A21280-100Darusentan 100mg
A21280-50Darusentan 50mg
A21280-2Darusentan 2mg
A21280-25Darusentan 25mg
A21280-1Darusentan 1mg
A21280-10Darusentan 10mg
A21280-10mM-DDarusentan 10mM * 1mL in DMSO

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