| 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: (2S)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid.
- Also known as: LU 135252
- CAS number: 171714-84-4
- Molecular formula: C22H22N2O6.
- Purity: >99%
- Concentration: 1 nM - 1 µM.
- Form: Lyophilized powder.
- Solubility: Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
- Reconstitution: Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
- 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: Darusentan is a selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with Ki of 6 nM and 371 nM, respectively1. in vitro Darusentan inhibits Endothelin-induced vascular contractility in isolated endothelium-denuded rat aortic rings with pA2 of 8.12. Darusentan is orally bioavailable and active in vivo3.
- Alternative names: LU 135252
Scientific background
Darusentan, (LU 135252), is a synthetic compound that acts as a selective antagonist of endothelin A (ET-A) receptors. Darusentan is orally bioavailable and is a potent inhibitor of vasoconstriction in large and small arteries. The compound is a propanoic acid based antagonist that consist of two enantiomers - (R) and (S). The (R) enantiomer shows no binding activity, indicating that the (S) enantiomer is the active drug1,2.in vitro, Darusentan inhibits endothelin-induced vascular contractility in isolated endothelium-denuded rat aortic rings with pA2 value of 8.11,2.Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also detected in several different regions of the brain3.
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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