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Submit ReviewGRI 977143
Description: Selective LPA2 receptor non-lipid agonist
Chemical Name: 2-[[3-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)propyl]thio]benzoic acid
Purity: ≥98% (HPLC)
Biological Activity for GRI 977143
GRI 977143 is a 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 for GRI 977143
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GRI 977143
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.14 | 100 |
Preparing Stock Solutions for GRI 977143
The following data is based on the product molecular weight 391.44. Batch specific molecular weights may vary from batch to batch due to the degree 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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Product Datasheets for GRI 977143
References for GRI 977143
References are publications that support the biological activity of the product.
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
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