GC 14
GC 14 is a selective thyroid hormone receptor antagonist, with IC50 values of 35 nM and 200 nM for hTRβ and hTRα, respectively.
For research use only. We do not sell to patients.
- CAS No.: 447415-34-1
- Formula: C26H27NO6
- Molecular Weight:449.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
In Vitro
GC 14 contains extensions at the 5′-position of the outer thyronine ring or from the bridging carbon and has only a modest affinity and potency for the thyroid hormone receptor (TR) that limits studies of their antagonistic actions[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 447415-34-1
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Molecular Weight 449.50
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Formula C26H27NO6
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SMILES
O=C(O)COC1=CC(C)=C(CC2=CC(C3=CC=C([N+]([O-])=O)C=C3)=C(O)C(C(C)C)=C2)C(C)=C1
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Purity & Documentation
References
[1]. Koehler K, et al. Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor. J Med Chem. 2006 Nov 16;49(23):6635-7. [Content Brief]
[2]. Chiellini G, et al. Synthesis and biological activity of novel thyroid hormone analogues: 5'-aryl substituted GC-1 derivatives. Bioorg Med Chem. 2002 Feb;10(2):333-46. [Content Brief]
[3]. Nguyen NH, et al. Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment. J Med Chem. 2002 Jul 18;45(15):3310-20. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)