M4 Human Acetylcholine (Muscarinic) GPCR GTPgammaS Antagonist LeadHunter Assay - TW

Item: 332000-1

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Muscarinic receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Muscarinic receptors are widely distributed in the central and peripheral nervous system as well as various tissues.

Family:

GPCR

Sub Family:

Acetylcholine (Muscarinic)

Class:

Class A

Protein Name:

Uniprot Number:

P08173

Protein Aliases:

acetylcholine receptor, muscarinic 4

Gene Name:

CHRM4

Gene ID:

1132

Accession Number:

NM_000741

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

GTPgammaS

Functional Mode:

Antagonist

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Incubation:

15 min at 30°C

Control Inhibitor:

4-Damp methiodide

Criteria For Significance:

≥ 50% Increase in bound [35S]GTPgammaS relative to McN-A-343 response, ≥ 50% Inhibition of McN-A-343-induced bound [35S]GTPgammaS

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

3014059

Name

4-DAMP

Measurement

19nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei