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Darusentan

Catalog No. T5458 CAS 171714-84-4

Synonyms: Lu-135252

Darusentan (Lu-135252) is a potent inhibitor of endothelin signaling and function in both large and small arteries

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Darusentan, CAS 171714-84-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
2 mg	In stock	$ 63.00
5 mg	In stock	$ 105.00
10 mg	In stock	$ 178.00
25 mg	In stock	$ 322.00
50 mg	In stock	$ 531.00
100 mg	In stock	$ 768.00
1 mL * 10 mM (in DMSO)	In stock	$ 108.00

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Purity: 97.26%

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Description	Darusentan (Lu-135252) is a potent inhibitor of endothelin signaling and function in both large and small arteries
In vitro	Darusentan inhibits endothelin-induced signaling related to pro-contractile activity and is a potent inhibitor of vasoconstriction in large and small arteries.
Cell Research	Briefly, isolated rat aortic smooth muscle cells were incubated overnight in complete media in a 96-well microplate at a density of 50 000 cells/well. The next day, cells were starved for 24 h in 0% serum conditions. Following starvation, medium was removed and cells were dosed with 20 μL of increasing concentrations of darusentan (0, 0.001, 0.01, 0.1, 1, and 10 μmol/L) made in stimulation buffer containing 50 mmol/L LiCl. Cells were incubated at 37 °C, 5% CO2 for 30 min before the addition of 20 μL of ET-1 in dose-response fashion. Cells were incubated in the presence or absence of darusentan and ET-1 at 37 °C, 5% CO2 for 60 min. Following this incubation, cells were lysed using 20 μL of 2.5% lysis solution for 30 min and lysates were transferred to a 96-well microplate pre-coated with goat anti-mouse IgG. After transfer into the ELISA plate, kit-supplied IP1-horseradish peroxidase (HRP) conjugate and anti-IP1 mAb were added to the lysates. Assays were incubated for 3 h at room temperature on a platform shaker. Assay plates were then washed 6 times with 1× ELISA wash solution (250 μL/well) before the addition of HRP substrate TMB (3, 3', 5, 5'-tetramethylbenzidine). After 20 min, the reaction was stopped and the optical density (OD) was measured at 450 nm with a correction of 620 nm. Measurements were performed in triplicate.

Synonyms	Lu-135252
Molecular Weight	410.43
Formula	C22H22N2O6
CAS No.	171714-84-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (304.57 mM)

H2O: Insoluble

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library GPCR Compound Library Anti-Cancer Drug Library Inhibitor Library Bioactive Compound Library Anti-Hypertension Compound Library Neurotransmitter Receptor Compound Library Bioactive Compounds Library Max Anti-Cardiovascular Disease Compound Library

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Keywords

Darusentan 171714-84-4 GPCR/G Protein Endothelin Receptor vascular ET-A Lu-135252 rat muscle Inhibitor Lu 135252 receptor aortic endothelin inhibit smooth RAVSMs Lu135252 inhibitor

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