Home GPCR & G Protein LPA Receptor antagonist Ki16198

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Ki16198 LPA Receptor antagonist

Cat.No.S2906

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 LPA Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 488.98

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Chemical Information, Storage & Stability

Molecular Weight 488.98 Formula

C24H25ClN2O5S

 Storage (From the date of receipt)
CAS No. 355025-13-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2Cl)C3=CC=C(C=C3)CSCCC(=O)OC

Solubility

In vitro
Batch:

DMSO : 98 mg/mL ( (200.41 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 98 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight

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

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Mechanism of Action

Targets/IC50/Ki
LPA1 [1]
0.34 μM(Ki)
LPA3 [1]
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. This compound (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. It (10 μM) inhibits the LPA-induced expression of proMMP-9 protein and mRNA in YAPC-PD cells. [1] This chemical (1 μM) inhibits the proliferation of lpa1Δ-1 and lpa1Δ+-1 cells by about 70%. [2]
Kinase Assay
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 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] This compound (60 mg/kg orally) significantly inhibits lactate-induced limb lesions in rats. [3]
References

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