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.
规格 | 价格 | 会员价 | 库存 | 数量 | |||
---|---|---|---|---|---|---|---|
{[ item.pr_size ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
产品名称 | LPA1 ↓ ↑ | LPA2 ↓ ↑ | LPA3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ki16198 |
+++
LPA1, Ki: 0.34 μM |
++
LPA3, Ki: 0.93 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
ONO-7300243 |
++++
LPA1, IC50: 0.16 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ki16425 |
+++
LPA1, Ki: 0.34 μM |
+
LPA2, Ki: 6.5 μM |
++
LPA3, Ki: 0.93 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
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。 |
靶点 |
|
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]. |
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 |
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 |