SML1550

Zibotentan

≥98% (HPLC)

• Synonyme(s) : N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulfonamide, ZD4054
• Formule empirique (notation de Hill): C₁₉H₁₆N₆O₄S
• Numéro CAS: 186497-07-4
• Poids moléculaire : 424.43
• Numéro MDL: MFCD09955343
• Code UNSPSC : 12352200
• ID de substance PubChem : 329825958

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 5 mg/mL, clear (warmed)
• Température de stockage: −20°C
• Chaîne SMILES: 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)
• Clé InChI: FJHHZXWJVIEFGJ-UHFFFAOYSA-N
• Informations sur le gène: human ... EDNRA(1909)

Description

Description générale

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

Actions biochimiques/physiologiques

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.

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H302
• Conseils de prudence: P264 - P270 - P301 + P312 - P501
• Classification des risques: Acute Tox. 4 Oral
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable