Biological Information

Background Information:

Adrenoreceptors 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. Adrenoreceptors are found in most peripheral tissue and within the central nervous system. Adrenergic a2C receptor may cause peripheral vasoconstriction; antagonism may act peripherally to increase the skeletal muscle blood flow.

Family:

GPCR

Sub Family:

Adrenoceptor

Class:

Class A

Protein Name:

alpha2C

Uniprot Number:

P18825

Protein Aliases:

Alpha-2C adrenoreceptor|Alpha-2C adrenoceptor|Alpha-2CAR

Gene Name:

ADRA2C

Gene ID:

152

Gene Aliases:

ADRA2L2|ADRA2RL2

Accession Number:

NM_000683

Organism:

Human

Construct Details:

Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

10 min at 37°C

Control Inhibitor:

rauwolscine

Control Activator:

epinephrine (30 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL testing. 2) Dose Response: 90 µL of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

4893

Name

Prazosin

Measurement

8700nM - IC50

PubChem ID

8969

Name

Yohimbine

Measurement

296nM - IC50

PubChem ID

108094

Name

2-Methoxyidazoxan

Measurement

268nM - IC50

PubChem ID

643606

Name

Rauwolscine

Measurement

36nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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