Biological Activity
Selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 μM). Does not activate other LPA GPCRs at concentrations up to 10 μM. Antiapoptotic; inhibits activation of caspases 3, 7, 8 and 9, Bax translocation and PARP-1 cleavage. Activates ERK1/2 survival pathway.
Technical Data
| M. Wt | 391.44 |
| Formula | C22H17NO4S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 325850-81-5 |
| PubChem ID | 3114900 |
| InChI Key | GMVZUCHUOYUMLL-UHFFFAOYSA-N |
| Smiles | O=C(C2=CC=CC3=CC=CC(C4=O)=C23)N4CCCSC1=CC=CC=C1C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.14 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 391.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.55 mL | 12.77 mL | 25.55 mL |
| 5 mM | 0.51 mL | 2.55 mL | 5.11 mL |
| 10 mM | 0.26 mL | 1.28 mL | 2.55 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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References
References are publications that support the products' biological activity.
Kiss et al (2012) Virtual screening for LPA2-specific agonists identifies a nonlipid compound with antiapoptotic actions. Mol.Pharmacol. 82 1162 PMID: 22968304
Kiss et al (2013) Mitigation of radiation injury by selective stimulation of the LPA(2) receptor. Biochim.Biophys.Acta 1831 117 PMID: 23127512
Keywords: GRI 977143, supplier, GRI977143, lysophospholipid, acid, 2, LPA2, inhibitors, inhibits, antiapoptotic, caspases, Bax, PARP-1, cleavage, ERK1/2, ERK, survival, pathway, apoptosis, Other, Apoptosis, Lysophosphatidic, Acid, Receptors, Lysophosphatidic, Acid, Receptors, Tocris Bioscience
