| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | Soluble in DMSO with gentle warming. Centrifuge all products before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: 5-(4-bromophenyl)-4-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-6-(sulfamoylamino)pyrimidine.
- Also known as: Despropyl Macitentan
- CAS number: 1103522-45-7
- Molecular formula: C16H14Br2N6O4S.
- Purity: >98%
- Concentration: 1-100 µM.
- Form: Lyophilized powder.
- Solubility: Soluble in DMSO with gentle warming. Centrifuge all products before use (10000 x g 5 min).
- Reconstitution: Soluble in DMSO with gentle warming. 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: Endothelin receptors
- Source: Synthetic
- Activity: ACT-132577, a metabolite of macitentan, is a dual antagonist of ET-A and ET-B endothelin receptors, inhibiting binding of 125I-ET-1 to recombinant ET-A and ET-B receptors with IC50 values of 3.4 nM and 987 nM, respectively1.
- Alternative names: Despropyl Macitentan
Scientific background
ACT-132577 is an active metabolite of Macitentan that acts as an endothelin B (ET-B) and endothelin A (ET-A) receptor antagonist. ACT-132577 antagonizes the specific binding of endothelin-1 on membranes of cells overexpressing ET-A and ET-B receptors with IC50 values of 3.4 nM and 987 nM, respectively1. It also has the ability to reach full inhibition of intracellular Ca2+ increase induced by endothelin-1 on non-recombinant cells1.Endothelin receptors belong to the superfamily of G-protein coupled receptors and include two subtypes: ET-A and ET-B. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also present in several different regions of the brain. ET-B receptors play an important role in regulating renal function and blood pressure and are expressed in sensory nerves. They are mainly detected in medium- and large-sized cell bodies of human trigeminal ganglia.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 isopeptides2,3.
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
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