Biological Information

Background Information:

VIP1 (VPAC1) 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. The VIP receptor family includes receptors for pituitary adenylate cyclase-activating polypeptide (PACAP), secretin, glucagon-like peptide-1 (GLP-1), calcitonin, parathyroid hormone and growth hormone-releasing factor, which are coupled preferentially to GaS to stimulate adenylate cyclase and increase cAMP levels. VIP1 receptors are widely distributed in the central nervous system, in peripheral tissues and in T lymphocytes.

Family:

GPCR

Sub Family:

VIP and PACAP

Class:

Class B

Protein Name:

VIP1 (VPAC1)

Uniprot Number:

P32241

Protein Aliases:

PVR2|HVR1|RDC1|VIP and PACAP receptor 1|PACAP-R2|pituitary adenylate cyclase-activating polypeptide type II receptor|VIP-R1

Gene Name:

VIPR1

Gene ID:

7433

Gene Aliases:

VPAC1|RDC1|HVR1|VPAC1R

Accession Number:

NM_004624

Organism:

Human

Cell Type:

HT-29

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

HTRF

Testing Information

Incubation:

10 min at 37°C

Control Activator:

VIP

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 final 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

16158474

Name

human secretin

Measurement

2190nM - EC50

PubChem ID

91935803

Name

PACAP1-38

Measurement

3.96nM - EC50

PubChem ID

16140438

Name

VIP

Measurement

0.4nM - EC50

PubChem ID

16133238

Name

PACAP 1-27

Measurement

0.35nM - EC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

VIP1 receptor agonism may reduce immune mediated brain, pulmonary and gastrointestinal inflammation, gastrointestinal transit and pulmonary hypertension and cause vasodilation.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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