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.
Biochem/physiol Actions
Primary Target
S1PR2
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C).
Other Notes
Satsu, H., et al. 2013. Bioorg. Med. Chem.21, 5373.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 345.39. Empirical Formula: C21H19N3O2. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51362001
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5313710001