- 商品介绍
- 规格参数
- 包装参数
General description
Zibotentan is an orally bioavailable, non-peptide ETA (endothelin) receptor-specific antagonist, with no activity against ETB 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.
Zibotentan is a potent and selective endothelin ET(A) receptor antagonist.
| Quality Segment | 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) |
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