Home GPCR & G Protein LPA Receptor antagonist Ki16198

Ki16198

Catalog No.S2906

For research use only.

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 Chemical Structure

CAS No. 355025-13-7

Selleck's Ki16198 has been cited by 1 Publication

1 Customer Review

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Biological Activity

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.
Targets
LPA1 [1] LPA3 [1]
0.34 μM(Ki) 0.93 μM(Ki)
In vitro

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. [1] Ki16198 (1 μM) inhibits the proliferation of lpa1Δ-1 and lpa1Δ+-1 cells by about 70%. [2]
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. [1] Ki16198 (60 mg/kg orally) significantly inhibits lactate-induced limb lesions in rats. [3]

Protocol (from reference)

Kinase Assay:[1]
  • 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.
Cell Research:[1]
  • Cell lines: YAPC-PD cells or Panc-1 cells
  • Concentrations: 10 μM
  • Incubation Time: 24 hours
  • Method: YAPC-PD cells or Panc-1 cells are seeded on 12-well plates at 1 × 104 cells in 1 mL. Sixteen hours before experiments, the medium is changed to RPMI1640 containing 0.1% BSA. Then, the cells are stimulated for 24 h in the same medium in the presence or absence of Ki16198. The proliferation activity is measured by the cellular ability to reduce MTT (3-(4,5-Dimethyl-2-thiazoyl)-2,5-diphenyltetrazolium bromide
  • (Only for Reference)
Animal Research:[1]
  • Animal Models: YAPC-PD xenograft mouse model
  • Dosages: 2 mg/kg
  • Administration: Orally
  • (Only for Reference)

Solubility (25°C)

In vitro

 DMSO 96 mg/mL
(196.32 mM)
Ethanol 35 mg/mL
(71.57 mM)
Water Insoluble

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.

 30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 488.98
Formula

C24H25ClN2O5S
CAS No. 355025-13-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2Cl)C3=CC=C(C=C3)CSCCC(=O)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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