GRI 977143

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Cat.No. 4779 - GRI 977143 | C22H17NO4S | CAS No. 325850-81-5
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)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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Keywords: GRI977143 lysophospholipid acid 2 LPA2 inhibitors inhibits antiapoptotic caspases Bax PARP-1 cleavage ERK1/2 ERK survival pathway apoptosis Lysophosphatidic Acid Receptors

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