Biological Information
Background Information:
Translocator protein (TSPO), previously called peripheral benzodiazepine receptor (PBR), was originally discovered as an alternative binding site for diazepam, a benzodiazepine. PBR/TSPO is a multimeric receptor composed of the Mr 18,000 receptor protein and the Mr 34,000 voltage-dependent anion channel protein. Expression of PBR has been found in every tissue examined; however, it is most abundant in steroid-producing tissues such as the adrenals, testes, ovaries, placenta, and brain, where it is primarily localized in the outer mitochondrial membrane. The primary function of PBR is the regulation of steroidogenesis, its existence in nonsteroidogenic tissues suggests that there may be other roles for PBR.
Family:
Mitochondrial Function
Sub Family:
Mitochondrial-Associated Protein
Protein Name:
PBR
Uniprot Number:
B1AH88|P30536
Protein Aliases:
peripheral-type benzodiazepine receptor/recognition site
Gene Name:
TSPO
Gene ID:
706
Gene Aliases:
PBR|MBR|PKBS|mDRC|DBI|IBP|pk18
Accession Number:
NM_007311
Organism:
Human
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H] PK 11195
Ligand Kd (nM):
5.3
Ligand Concentration:
0.5 nM
Non Specific:
10µM PK 11195
Incubation:
15 min at RT
Control Inhibitor:
PK 11195
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:
2
Turnaround Time
Standard:
10 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Cardiovascular
Adverse / Beneficial Action:
Agonist and/or antagonist may disturb steroidogenesis.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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