| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: 5-(dimethylamino)-N-(3,4-dimethyl-1,2-oxazol-5-yl)naphthalene-1-sulfonamide;hydrochloride.
- CAS number: 1215703-04-0
- Molecular formula: C17H19N3O3S · HCl
- Purity: >99%
- Concentration: 100 nM - 10 µM.
- Form: Lyophilized powder.
- Solubility: Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
- Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
- Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
- Target: ET-A receptors
- Source: Synthetic
- Activity: BMS 182874 hydrochloride is a potent, selective and competitive antagonist of ET-A endothelin receptors. It exhibits a 1000-fold selectivity for ET-A over ET-B receptors, inhibiting endothelin-1 radioligand binding to ET-A and ET-B with Ki of 61 nM and >50 µM, respectively. In vitro, BMS 182874 inhibits endothelin-1 induced calcium mobilization with KB of 140 nM1. BMS 182874 is orally bioavailable and active in vivo1,2.
Scientific background
BMS 182874 hydrochloride is a synthetic compound that acts as a selective, potent, and competitive antagonist of endothelin A (ET-A) receptors. BMS 182874 exhibits a 1000-fold selectivity for ET-A over ET-B receptors. The compound is a useful tool for understanding the role of endothelin in normal and disease conditions. BMS 182874 inhibits the binding of radioligand binding of ET-1 to ET-A receptors in rat vascular smooth muscle cell membranes with Ki of 61 nM and in Chinese ovary hamster cells with Ki of 48 nM1.Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues where they mediate vasoconstriction. They are also expressed in several different regions of the brain. The ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity for all endothelin isopeptides2.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.
- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
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- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
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