Biochem/physiol Actions

Reversible: yes

Primary TargetS1PR2

General description

A pyrrolyl ketone derivative that acts as a potent, selective, allosteric agonist of sphingosine-1-phosphate receptor 2 (S1PR2; EC₅₀ = 480 nM) that does not replace native ligand and its binding is not competitive with JTE-013. Does not affect the activity of S1PR1, 3, and 5 and the activity of 29 other receptors and transports in any significant manner. Acts as a full agonist for both wild type and triple mutant S1PR2 (EC₅₀ = 1.6 and 1.5 µM, respectively).

A pyrrolyl ketone derivative that acts as a potent, selective, allosteric agonist of sphingosine-1-phosphate receptor 2 (S1PR2; EC₅₀ = 480 nM) that does not replace native ligand and its binding is not competitive with JTE-013. Does not affect the activity of S1PR1, 3, and 5 and the activity of 29 other receptors and transports in any significant manner. Acts as a full agonist for both wild type and triple mutant S1PR2 (EC₅₀ = 1.6 and 1.5 µM, respectively).Please note that the molecular weight for this compound is batch-specific due to variable water content.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Satsu, H., et al. 2013. Bioorg. Med. Chem.21, 5373.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C).

Warning

Toxicity: Standard Handling (A)