Ogerin

Protein target name:

GPR68

Mechanism of action:

Positive Allosteric Modulator

Recommended Concentration for use in cells:

up to 1 uM

Probe Availability

MedChemExpress

TOCRIS

Sigma

Probe Information

Target and Probe Information

Target Details

Target class:

GPCR

Subclass:

Proton Sensing GPCR

HUGO ID:

HGNC:4519

Entrez gene ID:

8111

UNIPROT ID:

Q15743

Target alias:

OGR1, AI2A6, GPR12A

Probe Details

Chemical Probes Portal ID:

CPP1844

Probe alias:

ZINC67740571

PubChem CID:

56707820

SMILES string:

C1=CC=C(C=C1)CNC2=NC(=NC(=N2)N)C3=CC=CC=C3CO

InChi Key:

MDGIEDNDSFMSLP-UHFFFAOYSA-N

Control compound:

ZINC32547799

Physico-chemical properties

Solubility - preferred solvent:

DMSO 25-30 mg/ml

Solubility - concentration:

100 mM

NMR:

1H NMR (400 MHz, CD3OD) δ 7.97 – 7.88 (m, 1H), 7.46 (d, J = 3.9 Hz, 2H), 7.42 – 7.27 (m, 5H), 7.23 (t, J = 7.1 Hz, 1H), 4.65 (s, 2H), 4.62 (s, 2H).

13C NMR (101 MHz, CD3OD) δ 174.20, 168.19, 166.99, 141.52, 140.58,138.59, 131.65, 131.39, 130.91, 130.58, 129.46, 128.73, 128.43, 128.03, 64.59, 45.03.

Storage Recommendations

Storage (dry powder):

-20°C 3 years, 4°C 2 years

Storage (solution):

-80°C 6 months

Validation in Cells and Model Organisms

In vitro validation

Off target activity

Probe Selectivity in Vitro:

Screened for radioligand binding modulation of CNS GPCRs and toxic pharmacological off-targets. Minimal activity at all targets (pKi > 7)

In cell validation

On target activity in cells

Potency in cells:

pKbB

4.92

Potency assay (cells):

Glo cAMP assay analyzed using a 4-parameter logistic model for agonist activity (agonist: pH)

In vivo validation

Organism:

Mouse

Dose:

10 mg/Kg

Route of delivery:

Intraperitoneal

Organ of Interest

Organ (O):

Brain

Primary Reference

Reference (doi):

10.1038/nature15699

Reference (PMID):

26550826

External Resources

Available data:

SGC Chemical Probes

Ogerin

Probe Availability

Probe Information

Target Details

OGR1, AI2A6, GPR12A

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

In vivo validation

Primary Reference

External Resources

Supporting Organizations

Interested in supporting the portal?

Search form

Ogerin

Probe Availability

Probe Information

Target Details

OGR1, AI2A6, GPR12A

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

In vivo validation

Primary Reference

External Resources

Supporting Organizations

Interested in supporting the portal?