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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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Z125040-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $82.90 | |
Z125040-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $282.90 | |
Z125040-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $899.90 |
Synonyms | C19H16N6O4S | DB06629 | PDSP2_001599 | BROMPERIDOL DECANOATE [USP-RS] | Zibotentan [USAN:INN:JAN] | 3-Pyridinesulfonamide, N-(3-methoxy-5-methylpyrazinyl)-2-(4-(1,3,4-oxadiazol-2-yl)phenyl)- | NCGC00242479-03 | 3-PYRIDINESULFONAMIDE, N-(3-METHOXY-5-METHYL |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | 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 resu |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ANTAGONIST |
Mechanism of action | Endothelin receptor ET-A antagonist |
Note | 250mg卖完停产,不再备货 |
Product Description |
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.
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ALogP | 1.4 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide |
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INCHI | 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 |
Canonical SMILES | CC1=CN=C(C(=N1)OC)NS(=O)(=O)C2=C(N=CC=C2)C3=CC=C(C=C3)C4=NN=CO4 |
Isomeric SMILES | CC1=CN=C(C(=N1)OC)NS(=O)(=O)C2=C(N=CC=C2)C3=CC=C(C=C3)C4=NN=CO4 |
RTECS | UT7937700 |
PubChem CID | 9910224 |
Molecular Weight | 424.43 |
Wikipedia | Zibotentan |
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CAS Registry No. | 186497-07-4 |
PubChem CID | 9910224 |
ChEMBL Ligand | CHEMBL1628688 |
GPCRdb Ligand | zibotentan |
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Solubility | DMSO ≥12mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
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Pictogram(s) | GHS08, GHS09 |
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Signal | Danger |
Hazard Statements | H373:Causes damage to organs through prolonged or repeated exposure H411:Toxic to aquatic life with long lasting effects H360:May damage fertility or the unborn child |
Precautionary Statements | P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P405:Store locked up. P501:Dispose of contents/container to ... P260:Do not breathe dust/fume/gas/mist/vapors/spray. P391:Collect spillage. P203:Obtain, read and follow all safety instructions before use. P318:if exposed or concerned, get medical advice. P319:Get medical help if you feel unwell. |
RTECS | UT7937700 |
Starting at $89.90