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Home > Inhibitors & Agonists > GPCR > Lysophospholipid Receptor

Ki16198

  Cat. No.:  DC8889   Featured
Chemical Structure
355025-13-7
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Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 355025-13-7
Chemical Name: Methyl 3-({4-[4-({[1-(2-chlorophenyl)ethoxy]carbonyl}amino)-3-met Hyl-1,2-oxazol-5-yl]benzyl}sulfanyl)propanoate
Synonyms: Methyl 3-({4-[4-({[1-(2-chlorophenyl)ethoxy]carbonyl}amino)-3-met hyl-1,2-oxazol-5-yl]benzyl}sulfanyl)propanoate;Ki16198
SMILES: COC(=O)CCSCC1=CC=C(C=C1)C2=C(NC(=O)OC(C)C3C(Cl)=CC=CC=3)C(C)=NO2
Formula: C24H25N2O5Scl
M.Wt: 488.9837
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA1 and LPA3-induced inositol phosphate production with Ki values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo[1].
In Vivo: Ki16198 (oral administaion; 1 mg in 500 ul; 28 days) significantly decreases the degree of metastasis activity in Ki16198-treated mice. Similiar to liver, metastasis to lung and brain in mice is also observed[1]. Animal Model: Male BALB/c nude mice (6 weeks old)[1] Dosage: 1 mg in 500 ul Administration: Oral administaion; 28 days Result: Inhibited lung and liver metastasis in vivo.
In Vitro: Ki16198 (0-10 μM; 48 hours) is effective to inhibit migration and invasion responses to LPA with a potency similar to that of Ki16425. The inhibitory effects Ki16198 on the invasion response to LPA, but not to EGF in several pancreatic cancer cell lines, including Panc-1,CFPAC-1, and BxPC-3 cells[1]. Ki16198 (10 μM; 48 hours) signifivcantly decreases expression of proMMP-9 protein and mRNA expression in YAPC-PD cells[1].
References: [1]. Mayumi Komachi, et al. Orally active lysophosphatidic acid receptor antagonist attenuates pancreatic cancer invasion and metastasis in vivo. Cancer Sci. 2012 Jun;103(6):1099-104.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC8889 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.
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