SML1550

Zibotentan

≥98% (HPLC)

• Synonym(e): N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulfonamide, ZD4054
• Empirische Formel (Hill-System): C₁₉H₁₆N₆O₄S
• CAS-Nummer: 186497-07-4
• Molekulargewicht: 424.43
• MDL-Nummer: MFCD09955343
• UNSPSC-Code: 12352200
• PubChem Substanz-ID: 329825958
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 5 mg/mL, clear (warmed)
• Lagertemp.: −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)
• InChIKey: FJHHZXWJVIEFGJ-UHFFFAOYSA-N
• Angaben zum Gen: human ... EDNRA(1909)

Beschreibung

Allgemeine Beschreibung

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

Biochem./physiol. Wirkung

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.

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• H-Sätze: H302
• P-Sätze: P264 - P270 - P301 + P312 - P501
• Gefahreneinstufungen: Acute Tox. 4 Oral
• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable