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GRI 977143

Chemical Structure : GRI 977143

CAS No.: 325850-81-5

GRI 977143 (GRI977143;GRI-977143)

Catalog No.: PC-60890Not For Human Use, Lab Use Only.

A potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GRI 977143 is a potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM).
GRI 977143 also inhibits LPA3 with IC50 of 6.6 uM.
GRI 977143 reduces the activation of caspases 3, 7, 8 and 9 and inhibits PARP1 cleavage and DNA fragmentation in different extrinsic and intrinsic models of apoptosis in vitro.
GRI 977143 promotes carcinoma cell invasion of human umbilical vein endothelial cell monolayers and fibroblast proliferation.

Physicochemical Properties

M.Wt 391.44
Formula C22H17NO4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-((3-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl)thio)benzoic acid

References

1. Kiss GN, et al. Mol Pharmacol. 2012 Dec;82(6):1162-73.

2. Lin KH, et al. Sci Rep. 2016 May 31;6:27050.

3. Patil R, et al. Chem Biol. 2015 Feb 19;22(2):206-16.

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