An LPA2 receptor agonist
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GRI-977143

Item No. 21900

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[3-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)propyl]thio]-benzoic acid
CAS Number
325850-81-5
Molecular Formula
C22H17NO4S
Formula Weight
391.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:40): 0.025 mg/ml
λmax
232 nm
SMILES
O=C(O)C1=CC=CC=C1SCCCN2C(C3=C4C(C2=O)=CC=CC4=CC=C3)=O
InChi Code
InChI=1S/C22H17NO4S/c24-20-16-9-3-6-14-7-4-10-17(19(14)16)21(25)23(20)12-5-13-28-18-11-2-1-8-15(18)22(26)27/h1-4,6-11H,5,12-13H2,(H,26,27)
InChi Key
GMVZUCHUOYUMLL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    GRI-977143 is an agonist of G protein-coupled lysophosphatidic acid receptor 2 (LPA2) with an EC50 value of 3.3 μM in LPA2-transfected RH7777 cells.1 It is selective for LPA2, having no activity at LPA1, LPA3, LPA4, and LPA5 at concentrations up to 10 μM. GRI-977143 increases growth and reduces caspase-3 and -7 activation in LPA2-transduced MEF fibroblasts. It increases MM1 rat hepatoma cell invasion and inhibits apoptosis of IEC-6 cells induced by TNF-α, doxorubicin (Item No. 15007), or serum withdrawal. GRI-977143 also rescues apoptotic cells from γ-irradiation-induced injury in vitro and in vivo.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kiss, G.N., Fells, J.I., Gupte, R.D., et al. Virtual screening for LPA2-specific agonists identifies a nonlipid compound with antiapoptotic actions. Mol. Pharmacol. 82(6), 1162-1173 (2012).

    2. Kiss, G.N., Lee, S.-C., Fells, J., et al. Mitigation of radiation injury by selective stimulation of the LPA2 receptor. Biochim. Biophys. Acta 1831(1), 117-125 (2013).