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Ki16425 is an antagonist of the lysophosphatidic acid receptors LPA1 and LPA3. Ki16425 inhibits the LPA-induced Ca(2+) response in THP-1 cells, 3T3 fibroblasts and A431 cells. Ki16425 also inhibited LPA-induced long-term responses, including DNA synthesis and cell migration. Ki16425 reduced the LPA-induced activation of p42/p44 mitogen activated protein kinase (MAPK), while acting as a weak stimulator of p42/p44 MAPK on its own, properties typical of a protean agonist. Significantly, Ki16425 also reduced the NGF-induced stimulation of p42/p44 MAPK and inhibited NGF-stimulated neurite outgrowth.
| Molecular Weight | 474.96 |
| Formula | C23H23ClN2O5S |
| CAS Number | 355025-24-0 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related LPL Receptor Products |
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| Ki16198
Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6. |
| GSK-2018682
This compound belongs to the class of organic compounds known as n-alkylindoles. These are compounds containing an indole moiety that carries an alkyl chain at the 1-position. |
| H2L5186303
H2L5186303 is a potent and selective LPA2 receptor antagonist with an IC50 of 9 nM. |
| AM095 sodium
AM095 is a potent and selective, orally bioavailable antagonist of lysophosphatidic acid receptor1 (LPA1). |
| AM966
AM966 is a potent, selective and orally active LPA(1) receptor antagonist which inhibits lung fibrosis in the mouse bleomycin model. |
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