Ki16198

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ki16198 是 Ki16425 的甲酯，Ki16425 是一种 LPA 拮抗剂，可抑制 LPA1 和 LPA3 诱导的磷酸肌醇产生，Ki 分别为 0.34 μM 和 0.93 μM。

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 (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.Ki16198 (10 μM; 48 hours) signifivcantly decreases expression of proMMP-9 protein and mRNA expression in YAPC-PD cells.

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. Animal Model:Male BALB/c nude mice (6 weeks old) Dosage:1 mg in 500 ul Administration:Oral administaion; 28 days Result:Inhibited lung and liver metastasis in vivo.

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GPCR/G Protein

LPA Receptor

LPA1 LPA3

Cancer

Cancer

355025-13-7

488.98

C24H25ClN2O5S

>98% (HPLC)

DMSO:89 mg/mL (182 mM);Ethanol:33 mg/mL (67.5 mM);Water:<1 mg/mL

COC(=O)CCSCC1=CC=C(C=C1)C1=C(NC(=O)OC(C)C2=C(Cl)C=CC=C2)C(C)=NO1

3-(4-(4-((1-(2-Chlorophenyl)ethoxy)carbonylamino)-3-methyl-5-isoxazolyl)benzylsulfanyl)propanoic acid methyl ester

(-20℃)

With Ice Pack

≥ 2 years