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CAS No. 355025-13-7
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.
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Pain behavior and EDG2 and Nav1.8 expression after intrathecal injection of LPA. A LPA decreased PWTs (n = 8), and this was attenuated by the EDG2 antagonist Ki16198. B, C LPA up regulated EDG2 expression in L4-6 DRGs (n = 6). D, E Nav1.8 expression on L4-6 DRGs increased after LPA injection (n = 6). *P<0.05, **P<0.01, ***P<0.001.
Neurosci Bull, 2016, 32(5):445-54.. Ki16198 purchased from Selleck.
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|Description||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.|
Ki16198 or Ki16425 substantially inhibits LPA1- and LPA3-mediated responses with a similar potency, with low potency to LPA2 and no activity to LPA4, LPA5 and LPA6. Ki16198 (10 μM) is also effective to inhibit migration and invasion responses to LPA in YAPC-PD cancer cell line with a potency similar to that of Ki16425. Ki16198 (10 μM) inhibits the LPA-induced expression of proMMP-9 protein and mRNA in YAPC-PD cells.  Ki16198 (1 μM) inhibits the proliferation of lpa1Δ-1 and lpa1Δ+-1 cells by about 70%. 
|In vivo||Ki16198 (2 mg/kg) significantly decreases the total metastatic node weight in the peritoneal cavity and ascites formation by 50% in YAPC-PD xenograft mouse model.  Ki16198 (60 mg/kg orally) significantly inhibits lactate-induced limb lesions in rats. |
Inositolphosphate response:RH7777 cells expressing LPA1, LPA2, LPA3, LPA4, or LPA5 are cultured on collagen-coated 12-well dishes in the growth medium, and then the medium is changed to TCM199 containing 2 μCi/mL [3H]inositol and 0.1% (w/v) BSA (fraction V). After 24 h later, the cells are washed three times with HEPES-buffered medium, which consisted of 20 mM Hepes (pH 7.4), 134 mM NaCl, 4.7 mM KCl, 1.2 mM KH2PO4, 1.2 mM MgSO4, 2 mM CaCl2, 2.5 mM NaHCO3, 5 mM glucose, and 0.1% (w/v) BSA, and incubated for 30 min with the indicated concentrations of Ki16425 or Ki16198 with or without 1 μM LPA in the presence of 10 mM LiCl in the same medium at final volume of 0.5 mL. The reaction is terminated by adding 1 N HCl (0.1 mL) and freezing the cells. The supernatant (acid extract in 0.5 mL) of the thawed cells is used for the separation of [3H]inositol phosphate fractions. The results are normalized to 105 dpm of the total radioactivity incorporated into the cellular inositol lipids. The radioactivity of the trichloroacetic acid (5%)-insoluble fraction is measured as the total radioactivity.
|In vitro||DMSO||96 mg/mL (196.32 mM)|
|Ethanol||35 mg/mL (71.57 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
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Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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