Product Details
| Product Name:
Darusentan |
CAS No.:
171714-84-4 |
| Purity:
98.72% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | Darusentan |
| Description | Darusentan (Lu-135252) is a potent inhibitor of endothelin signaling and function 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. |
| In vitro | Darusentan inhibits endothelin-induced signaling related to pro-contractile activity and is a potent inhibitor of vasoconstriction in large and small arteries. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 125 mg/mL (304.57 mM)
H2O : Insoluble
|
| Keywords | vascular | ET-A | muscle | Inhibitor | Lu 135252 | receptor | aortic | inhibit | smooth | RAVSMs | Darusentan | Lu135252 | endothelin | rat | Endothelin Receptor |
| Inhibitors Related | Bosentan | BMS 182874 hydrochloride | Sulfisoxazole | Ambrisentan | Sparsentan | Aprocitentan |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States