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Darusentan

Darusentan

Item no.	HY-15404-10mg
Manufacturer	MedChem Express
CASRN	171714-84-4
Amount	10 mg
Quantity options	100 mg 10 mM/1 mL 10 mg 1 mg 25 mg 50 mg 5 mg
Category	Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Purity	98.67
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.
Smiles	COC1=NC(O[C@H](C(O)=O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)=NC(OC)=C1
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	Lu-135252
Similar products	171714-84-4
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	COVID-19-immunoregulation
Manufacturer - Targets	Endothelin Receptor
Shipping Temperature	Room Temperature
Storage Conditions	-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight	410.42
Product 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].
Manufacturer - Research Area	Cardiovascular Disease; Endocrinology
Solubility	DMSO: 100 mg/mL (ultrasonic)
Manufacturer - Pathway	GPCR/G Protein
Isoform	ETA
Clinical information	Phase 3

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HY-15404-10mg-safety-datasheet.pdf