Tetronothiodin
Tetronothiodin is a selective CCKB receptor antagonist. Tetronothiodin inhibits rat CCKB receptor binding with an IC50 of 3.6 nM and human CCKB receptor binding with an IC50 of 210 nM, exhibiting species specificity. Tetronothiodin inhibits CCK-induced Ca2+ influx in pituitary cells. Tetronothiodin can be used in research related to CCKB-mediated diseases.
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- CAS. Nr.: 139643-79-1
- Formel: C31H38O8S
- Molecular Weight:570.69
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
CCKBR 3.6 nM (IC50) |
In Vitro
Tetronothiodin inhibits the binding of [125I]CCK-8 to CCKB-rich regions of the rat forebrain in a concentration-dependent manner, almost completely abolishing binding at 1 µM, with the exception of the medial septum[1].
Tetronothiodin inhibits the binding of [125I]-CCK-8 to GH3 cells, with an IC50 of 4.2 nM[1].
Tetronothiodi is a selective CCKB antagonist in GH3 rat anterior pituitary cells that inhibits CCK-8-induced Ca2+ mobilization with an IC50 of 26 nM[1].
Tetronothiodin binds to rat brain cortex CCK-B receptors in the 125I-CCK-8 displacement assay with an IC50 of 3.6 nM; it binds to human CCK-B receptors with an IC50 of 210 nM, which is weaker than its activity against rat CCK-B receptors[2].
Tetronothiodin can be produced by Streptomyces sp. NR0489[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 139643-79-1
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Molecular Weight 570.69
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Formel C31H38O8S
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SMILES
O=C(C(C1SCC2C(C3=C(O)C4(CC(C)C(C)=CC4C/C=C\C=C/CC(C/C=C/CC(C12)C)O)OC3=O)=O)=O)O
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Synonyms
Ro 09-1468
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Initial Source
Streptomyces sp. NR0489
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Keywords
- Tetronothiodin
- 139643-79-1
- Ro 09-1468
- Cholecystokinin Receptor
- Endogenous Metabolite
- CCK Receptor
- CCK_A receptor
- CCK_B receptor
- GH3 cells
- Streptomyces sp. NR0489
- anterior pituitary tumor cell line
- cholecystokinin
- cytosolic calcium mobilization
- forebrain
- medial septal nucleus
- rat cerebral cortex membranes
- Inhibitor
- inhibitor
- inhibit