Zibotentan

SKU:BHB21300383
Overview
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Zibotentan (CAS 186497-07-4) 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). Supplied as Lyophilized powder (purity >95%, solubility Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min)). Commonly used in Molecular & Cellular Biology studies, including binding assays and second-messenger readouts.
Target ET-A receptor
Cas No 186497-07-4
concentration 1 nM - 10 µM.
purity >95%
Molecular Formula C19H16N6O4S.
Form Lyophilized powder.
Options selector
Catalog no. Size Quantity
Z-130-10MG-1 10 mg
Z-130-100MG-1 100 mg
Z-130-25MG-1 25 mg
Z-130-5MG-1 5 mg
Z-130-50MG-1 50 mg
Available Options

Select the variant that best fits your experiment. Availability and lead time may vary by option.

  • Options: Size (5) - 10 mg, 100 mg, 25 mg, 5 mg, 50 mg; Quantity: 1
  • Lead time: typically ships in 1-2 business days; timing may vary by selected option.
  • Storage: Storage of solutions: Up to three months at -20°C.
  • 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.
  • Upon receipt: store at the recommended temperature as soon as possible.
  • Sales terms and conditions: Please review prior to ordering.
Field Specification
Mfr No Z-130
Activity
  • Antagonist
Cas No. 186497-07-4
Concentration 1 nM - 10 µM.
Form Lyophilized powder.
Product Type
  • Biochemicals
  • Small Molecules
Purity >95%
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.
Solubility Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Source Synthetic
Storage Storage of solutions: Up to three months at -20°C.
Target ET-A receptor

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

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
  • Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
  • 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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Experience the power of Celltrypse™, c-LEcta's innovative enzyme solution for gentle and efficient cell dissociation. Request your free sample and discover a superior alternative for your cell culture workflows.

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