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.
For research use only. We do not sell to patients.
- CAS No.: 139643-79-1
- Formula: C31H38O8S
- Molecular Weight:570.69
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Endogenous Metabolite Isoforms
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Biological Activity
Description
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 No. 139643-79-1
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Molecular Weight 570.69
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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