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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >GPCR & G Protein >Endothelin Receptor Antagonists >Zibotentan (ZD4054)

Zibotentan (ZD4054)

Zibotentan (ZD4054) Structure
  • ₹0
  • Product name: Zibotentan (ZD4054)
  • CAS: 186497-07-4
  • MF: C19H16N6O4S
  • MW: 424.43
  • EINECS:
  • MDL Number:MFCD09955343
  • Synonyms:N-(3-METHOXY-5-METHYLPYRAZIN-2-YL)-2-[4-(1,3,4-OXADIAZOL-2-YL)PHENYL]PYRIDINE-3-SULFONAMIDE;3-Pyridinesulfonamide, N-(3-methoxy-5-methylpyrazinyl)-2-(4-(1,3,4-oxadiazol-2-yl)phenyl)-;Zd 4054;Zd4054;Zibotentan;Zibotentan(ZD4054);N-(3-Methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-3-pyridinesulfonamide;2-(4-(1,3,4-oxadiazol-2-yl)phenyl)-N-(3-Methoxy-5-Methylpyrazin-2-yl)pyridine-3-sulfonaMide
Properties Safety Information Description
Manufacturer Product number Product description Packaging Price Updated Buy

Properties

Melting point :239 - 241°C
Boiling point :637.0±65.0 °C(Predicted)
Density :1.422
storage temp. :Sealed in dry,Store in freezer, under -20°C
solubility :DMSO (Sparingly), Methanol (Slightly)
form :Solid
pka :5.62±0.40(Predicted)
color :White to Off-White

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning GHS hazard pictograms P264, P270, P301+P312, P330, P501
Precautionary statements:

Description

Zibotentan is a selective antagonist of the endothelin (ET) receptor type A (IC50s = 21 and >10,000 nM for human recombinant ETA and ETB, respectively). It inhibits growth of HEY, OVCA 433, SKOV3, and A2780 cells induced by endothelin 1 (ET-1; ) in vitro. Zibotentan reduces ET-1-induced expression of MMP-2, MMP-9, VEGF, COX-1 and COX-2, mediators of cell invasion and angiogenesis, in HEY cells. In vivo, zibotentan (10-50 mg/kg per day) reduces tumor growth in an HEY mouse xenograft model in a dose-dependent manner. Formulations containing zibotentan are under clinical investigation for the treatment of ovarian and castration-resistant prostate cancers.

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