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Ki16198 {[allProObj[0].p_purity_real_show]}

货号:A666171 Ambeed 开学季,买赠积分,赢豪礼

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 化学结构 CAS号:355025-13-7
Ki16198 化学结构
CAS号:355025-13-7
Ki16198 3D分子结构
CAS号:355025-13-7
Ki16198 化学结构 CAS号:355025-13-7
Ki16198 3D分子结构 CAS号:355025-13-7
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Ki16198 纯度/质量文件 产品仅供科研

货号:A666171 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 LPA1 LPA2 LPA3 其他靶点 纯度
Ki16198 +++

LPA1, Ki: 0.34 μM

++

LPA3, Ki: 0.93 μM

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ONO-7300243 ++++

LPA1, IC50: 0.16 μM

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Ki16425 +++

LPA1, Ki: 0.34 μM

+

LPA2, Ki: 6.5 μM

++

LPA3, Ki: 0.93 μM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Ki16198 生物活性

靶点
  • LPA1

    LPA1, Ki:0.34 μM

  • LPA3

    LPA3, Ki:0.93 μM

描述 Ki16198 is a potent and orally active antagonist of LPA receptors, functioning as the methyl ester derivative of Ki16425. It demonstrates efficacy in inhibiting LPA1 and LPA3-induced inositol phosphate production, with Ki values of 0.34 μM and 0.93 μM, respectively, showcasing its potential against pancreatic cancer tumorigenesis and metastasis when applied in vivo[1].
体内研究

Oral administration of Ki16198 (1 mg in 500 μl for 28 days) significantly reduces metastasis activity in treated mice, showing a notable decrease in metastatic spread to the liver, lungs, and brain. This highlights Ki16198's broad therapeutic potential in mitigating metastasis across multiple organ systems[1].

体外研究

In vitro experiments reveal that Ki16198, across a concentration range of 0 to 10 μM over 48 hours, effectively curtails migration and invasion responses to LPA in a manner comparable to Ki16425. Specifically, Ki16198 impacts the invasion response to LPA, without affecting responses to EGF, across various pancreatic cancer cell lines such as Panc-1, CFPAC-1, and BxPC-3[1].

At a concentration of 10 μM over 48 hours, Ki16198 markedly reduces both the protein and mRNA expression levels of proMMP-9 in YAPC-PD cells, indicating its role in modulating enzymes involved in cancer progression[1].

Ki16198 参考文献

[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.

Ki16198 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.20mL

10.23mL

2.05mL

1.02mL

20.45mL

4.09mL

2.05mL

Ki16198 技术信息

CAS号355025-13-7
分子式C24H25ClN2O5S
分子量 488.984
别名
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(214.73 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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