TR Beta Human Thyroid Hormone NHR Binding Agonist Radioligand LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Thyroid hormone receptors are members of a superfamily of nuclear receptors that transduce the effects of a diverse array of small, hydrophobic ligands, including the steroid hormones, thyroid hormone, vitamin D and retinoids. Thyroid hormones increase protein synthesis in virtually every body tissue, influence basal calorigenesis and O2 consumption in liver, kidney, heart, and skeletal muscle. Thyroid hormone receptors are recognized -- TR α and β. Thyroid hormone receptor agonists are used clinically for the treatment of thyroid gland deficiency diseases in adults, cretinism in children; higher doses may cause thyrotoxicosis. Antagonists may cause bradycardia, increased peripheral vascular resistance, elevation of mean blood pressure and hypercholesteremia.
Family:
NHR
Sub Family:
Thyroid Hormone
Class:
Non-Steroid
Protein Name:
THRB
Uniprot Number:
P10828
Protein Aliases:
Nuclear receptor subfamily 1 group A member 2
Gene Name:
THRB
Gene ID:
7068
Accession Number:
NP_000452.2
Organism:
Human
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant thyroid receptors β expressed in insect cells are used in modified Tris-HCl buffer pH 7.6. A 0.625 ngǂ aliquot is incubated with 0.06 nM [¹²⁵I]Triiodothyronine for 24 hourss at 4℃. Non-specific binding is estimated in the presence of 1 mM Triiodothyronine. Membranes are filtered and washed, the filters are then counted to determine [¹²⁵I]Triiodothyronine specifically bound. Compounds are screened at 10 µM.
Ligand:
[¹²⁵I] Triiodothyronine
Ligand Kd (nM):
0.21
Ligand Concentration:
0.06 nM
Non Specific:
1 µM Triiodothyronine
Incubation:
20 hrs at 4°C
Control Inhibitor:
Triiodothyronine
Criteria For Significance:
≥ 50% of max stimulation or inhibition≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
Metabolic Dysfunction-Associated Steatohepatitis (MASH) LeadHunter Panel - TW
Item: PP318
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