| 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: N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide.
- Also known as: ZD4054
- CAS number: 186497-07-4
- Molecular formula: C19H16N6O4S.
- Purity: >95%
- Concentration: 1 nM - 10 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: Zibotentan is a selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to human ET-A with IC50 of 21 nM (whilst showing no effect on ET-B at 10 µM). Zibotentan is orally bioavailable and active in vivo.1
- Alternative names: ZD4054
Scientific background
Zibotentan (ZD4054) is an orally active nonpeptide with specificity towards Endothelin A (ET-A) receptors with no activity on Endothelin B (ET-B) receptors. The compound inhibits endothelin-1 radioligand binding to human ET-A receptor with an IC50 value of 21 nM1.Studies show that Zibotentan successfully inhibits growth of tumor xenografts in mice and enhances the cytotoxicity of paclitaxel in ovarian carcinoma in vitro and in vivo1.Endothelin receptors 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 present in several regions of the brain. ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-32.
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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- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
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