SML1550

Zibotentan

≥98% (HPLC)

• Synonym(s): N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulfonamide, ZD4054
• Empirical Formula (Hill Notation): C₁₉H₁₆N₆O₄S
• CAS Number: 186497-07-4
• Molecular Weight: 424.43
• MDL number: MFCD09955343
• UNSPSC Code: 12352200
• PubChem Substance ID: 329825958
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 5 mg/mL, clear (warmed)
• storage temp.: −20°C
• SMILES string: O=S(C1=C(C2=CC=C(C3=NN=CO3)C=C2)N=CC=C1)(NC4=NC=C(C)N=C4OC)=O
• InChI: 1S/C19H16N6O4S/c1-12-10-21-17(19(23-12)28-2)25-30(26,27)15-4-3-9-20-16(15)13-5-7-14(8-6-13)18-24-22-11-29-18/h3-11H,1-2H3,(H,21,25)
• InChI key: FJHHZXWJVIEFGJ-UHFFFAOYSA-N
• Gene Information: human ... EDNRA(1909)

Description

General description

Zibotentan is an orally bioavailable, non-peptide ET_A (endothelin) receptor-specific antagonist, with no activity against ET_B receptor.

Biochem/physiol Actions

Zibotentan has been found to inhibit cell proliferation, invasion and metastasis in cancer models. In clinical trials on patients with castration-resistant prostate cancer and bone metastasis, who were pain-free or had mild pain, zibotentan treatment resulted in better overall survival as compared to placebo.

Zibotentan is a potent and selective endothelin ET(A) receptor antagonist with an IC₅₀ of 21 nM for the ETA receptor subtype and no binding observed even at 10,000 nM for ETB.

Safety Information

• Pictograms: GHS07
• Signal Word: Warning
• Hazard Statements: H302
• Precautionary Statements: P264 - P270 - P301 + P312 - P501
• Hazard Classifications: Acute Tox. 4 Oral
• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable