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  3. Ki16198

Ki16198 

目录号: HY-18641
产品使用指南

Ki16198 是一种口服活性强的 LPA 受体 (LPA receptor) 拮抗剂,是 Ki16425 (HY-13285) 的甲酯衍生物。Ki16198 对 LPA1 和 LPA3 诱导的肌醇磷酸的抑制作用 Ki 值分别为 0.34 μM 和 0.93 μM。Ki16198 在小鼠模型中对胰腺癌发生和转移有明显的作用。

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Ki16198 Chemical Structure

Ki16198 Chemical Structure

CAS No. : 355025-13-7

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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].

IC50 & Target

Ki: 0.34 μM (LPA1 receptor)
Ki: 0.93 μM (LPA1 receptor)[1]

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].

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.
Molecular Weight

488.98

Formula

C₂₄H₂₅ClN₂O₅S

CAS No.

355025-13-7

SMILES

O=C(OC)CCSCC1=CC=C(C2=C(NC(OC(C3=CC=CC=C3Cl)C)=O)C(C)=NO2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

Ki16198Ki 16198Ki-16198LPL ReceptorLysophospholipid Receptorlungliver metastasisPanc-1,CFPAC-1BxPC-3Inhibitorinhibitorinhibit

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产品名称:
Ki16198
目录号:
HY-18641
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