IR (INSR) Rat RTK Kinase Binding Radiometric LeadHunter Assay Agonist Radioligand - TW

Item: 243000

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Insulin receptors are present in virtually all mammalian cells, including targets classic for insulin action in regulation of fuel metabolism (liver, muscle and fat cells) as well as nonclassic targets (circulating blood, brain and gonadal cells). The insulin receptor and receptors for several other growth factors including epidermal growth factor (EGF), platelet-derived growth factor (PDGF), etc., are ligand-activated tyrosine protein kinases, which are required for signal transduction. Insulin receptor agonism may be useful in the treatment of hyperglycemic insulin-dependent diabetes or non-insulin-dependent diabetes mellitis (IDDM or type I diabetes and NIDDM, respectively); excessive receptor stimulation may cause hypoglycemia resulting in sweating, paresthesias, palpitations, tremors, anxiety, dizziness, weakness, loss of conciousness, etc.

Family:

Kinase

Sub Family:

RTK

Class:

Protein Tyrosine

Protein Name:

Uniprot Number:

P06213

Protein Aliases:

CD antigen CD220 [Cleaved into: Insulin receptor subunit alpha; Insulin receptor subunit beta]

Gene Name:

INSR

Gene ID:

3643

Gene Aliases:

CD220

Organism:

Rat

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Liver of male Wistar derived rats weighing 175 ± 25 g are used to prepare insulin receptors in modified Na-K phosphate buffer pH 7.4. A 3 mg‡ aliquot is incubated with 30 pM [¹²⁵I]Insulin for 16 hours at 4°C. Non-specific binding is estimated in the presence of 1 μM insulin. Membranes are filtered and washed, the filters are then counted to determine [¹²⁵I]Insulin specifically bound. Compounds are screened at 10 μM.
Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary.

Ligand:

[¹²⁵I] Insulin

Ligand Kd (nM):

0.47

Ligand Concentration:

0.03 nM

Non Specific:

1 µM Insulin

Incubation:

960 min at 4°C

Control Inhibitor:

Insulin

Criteria For Significance:

≥ 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:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

Name

Insulin

Measurement

0.0011μM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei