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Ki16425(Debio 0719)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ki16425(Debio 0719)图片
CAS NO:355025-24-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)474.96
FormulaC23H23ClN2O5S
CAS No.355025-24-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 94 mg/mL (197.9 mM)
Water: <1 mg/mL
Ethanol: 94 mg/mL (197.9 mM)
Solubility (In vivo)5% DMSO+95% Corn oil: 30 mg/mL
SynonymsKi16425; Debio0719; Ki-16425; Debio 0719; Ki 16425; Debio-0719
实验参考方法
In Vitro

In vitro activity: Kil6425 preferentially inhibits LPA1- and LPA3-mediated responses but has only a moderate effect on LPA2. Ki16425 inhibits the LPA-induced Ca(2+) response in THP-1 cells, 3T3 fibroblasts, and A431 cells, but had only a marginal effect in PC-12 cells and HL-60 cells, which means that Ki16425 seems to be a useful tool for evaluating the involvement of specific LPA receptors in the short-term response to LPA. Ki16425 inhibits long-term DNA synthesis and cell migration as induced by LPA in Swiss 3T3 fibroblasts. Ki16425 reduces the LPA-induced activation of p42/p44 mitogen activated protein kinase (MAPK), while acting as a weak stimulator of p42/p44 MAPK on its own, properties typical of a protean agonist. Ki16425 also significantly reduces the NGF-induced stimulation of p42/p44 MAPK and inhibited NGF-stimulated neurite outgrowth in PC-12 cells. Ki16425 markedly inhibits the expressions of COX-2 protein induced by synovial fluids. The enhancement of the IL-1 action by LPA on COX-2 expression is also inhibited by Ki16425.


Kinase Assay: RH7777 cells are incubated for 1 min with or without Ki16425, and the inositol phosphates (sum of inositol bisphosphate and inositol trisphosphate) were measured. The results were normalized to 105 dpm of the total radioactivity incorporated into the cellular inositol lipids, and the radioactivity of trichloroacetic acid (5%)-insoluble fraction was considered as the total radioactivity.


Cell Assay: In human breast and prostate cancer cells, Ki16425 inhibited heparin-binding EGF-like growth factor (HB-EGF) expression.

In VivoKi-16425 (30 mg/kg, i.p.) completely blocks LPA-induced neuropathic pain-like behaviors, when administered 30 min but not 90 min before lysophosphatidic acid injection, suggesting that Ki-16425 is a short-lived inhibitor. Ki-16425 also inhibits nerve injury-induced up-regulation of Caα2δ-1 in the dorsal root ganglion and reduction of SP immunoreactivity in the spinal dorsal horn.
Animal modelMale standard ddY-strain mice
Formulation & DosageDissolved in sesame oil; 30 mg/kg; i.p. administration.
References

Mol Pharmacol. 2003 Oct;64(4):994-1005; J Neurochem. 2006 Sep;98(6):1920-9; J Neurochem. 2009 Apr;109(2):603-10.