Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively, shows 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 | LPA (lysophosphatidic acid), which has been shown to be involved in certain diseases such as atherosclerosis and cancer, can act through its receptor like LPA receptor 1, LPA receptor 2, or LPA receptor 3 and elicit different biological actions, like Ca2+ mobilization, changing in cAMP accumulation, changing cell shape and motility, and cell proliferation. Ki16425 is a LPA receptor antagonist with Ki values of 0.34μM for mouse LPA receptor 1 and 0.93μM for human LPA receptor 3, but with much higher Ki value for human LPA receptor 2 (Ki=6.5μM). Pre-treatment with 1μM Ki16425 can inhibit LPA-induced [Ca22+]i increase in THP-1 cells and 3T3 fibroblasts. Also, Ki16425 could decrease the This LPA-induced response of inositol phosphate production in 3T3 fibroblasts and A431 cells, but not S1P3- or S1P2-expressing CHO cells, at concentration of 10μM. The cAMP accumulation inhibited by LPA in FRTL-5 thyroid cells in a PTX-sensitive manner could be almost completely suppressed by 10μM Ki16425. Cell proliferation and migration induced by LPA in Swiss 3T3 fibroblasts could be inhibited dose-dependently by Ki16425. Treatment with Ki16425 at dose of 10mg/kg intradermally could improve dermal and lung fibrosis in a mouse model of bleomycin-induced murine scleroderma. Pre-treatment with 10μM for 30 minutes could completely block LPA-induced YAP/TAZ phosphorylation and inhibit Hippo signaling pathway in HEK293A cells. |
作用机制 | Ki16425 can antagonize the binding of LPA to the receptor, thus competitively inhibiting LPA-induced GTP binding and LPA receptor binding to membrane fractions.[1] |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
CHOK1 cells | Function assay | Antagonist activity at human recombinant LPA1 receptor expressed in CHOK1 cells assessed as inhibition of lysophosphatidic acid-induced intracellular calcium influx, IC50=0.51 μM | 17467986 | ||
HEK293 cells | Function assay | 5 mins | Antagonist activity at human LPA1 receptor expressed in HEK293 cells assessed as inhibition of LPA-induced AP-TGF-alpha release treated 5 mins before LPA addition measured after 60 mins | 22658556 | |
human chem1 cells | Function assay | Antagonist activity at LPA1 expressed in human chem1 cells assessed as effect on intracellular calcium mobilization by FLIPR assay, IC50=0.046 μM | 20056548 | ||
PC-3 cells | Function assay | Binding affinity for Lysophosphatidic acid receptor in PC-3 cells, Ki=1.74 μM | 16033271 | ||
Dose | Mice: 1 mg/kg, 10 mg/kg[2] (i.d.); 20 mg/kg[4] (i.p.); 5 mg/kg[5] (i.v.); 25 mg/kg, 50 mg/kg[5] (p.o.) | ||||||||||||||||
Administration | i.d., i.p., i.v., p.o. | ||||||||||||||||
Pharmacokinetics |
|
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.11mL 0.42mL 0.21mL |
10.53mL 2.11mL 1.05mL |
21.05mL 4.21mL 2.11mL |
CAS号 | 355025-24-0 |
分子式 | C23H23ClN2O5S |
分子量 | 474.957 |
别名 | Debio 0719 |
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(221.07 mM),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 |