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FR 180204
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。
FR 180204图片
CAS NO:865362-74-9
规格:≥98%
包装与价格:
包装价格(元)
5mg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)327.34
FormulaC18H13N7
CAS No.865362-74-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 65 mg/mL (198.6 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL warmed (6.1 mM)
Other infoChemical Name: 5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-amine
InChi Key: XVECMUKVOMUNLE-UHFFFAOYSA-N
InChi Code: InChI=1S/C18H13N7/c19-17-12-10-13(20-22-18(12)23-21-17)15-14-8-4-5-9-25(14)24-16(15)11-6-2-1-3-7-11/h1-10H,(H3,19,21,22,23)
SMILES Code: NC1=NNC2=NN=C(C3=C4C=CC=CN4N=C3C5=CC=CC=C5)C=C21
SynonymsFR-180204; FR 180204; FR180204.
实验参考方法
In Vitro

In vitro activity: In AP-1-transfected cells, FR180204 dose-dependently inhibits AP-1 transactivation with IC50 of 3.1 μM. FR 180204 inhibits spontaneous mesothelioma cell growth.


Kinase Assay: Nunc-Immuno MaxiSorp plates are coated with 20 μg/ml MBP solution in phosphate-buffered saline (PBS). After washing with PBS containing 0.05% Tween 20 (T-PBS), blocking buffer (T-PBS containing 3% BSA) is added to each well and the plates are incubated for 10 min at room temperature. After washing with T-PBS, chemical compounds, ATP and recombinant ERK2 diluted in assay dilution buffer (20 mM Mops, pH 7.2, 25 mM β-glycerol phosphate, 5 mM EGTA, 1 mM sodium orthovanadate, 1 mM dithiothreitol, and 50 μg/ml BSA) and are added to each well. Vehicle groups (containing 0.1% DMSO) and kinase-withdrawal groups are used for the control and basal determinations. After incubation for 1 h at room temperature, plates are washed twice with T-PBS. Anti-phospho MBP antibody (0.2 μg/ml) is added to each well, and the plates are incubated for 1 h at room temperature. After washing, anti-mouse HRP-conjugated polyclonal antibodies are added and the plates were incubated for 30 min. SuperSignal chemiluminescent substrate is used for the measurement of HRP activity according to the manufacturer’s instructions. Prism 4.0 software is used for the Lineweaver–Burk plot analysis, IC50 and Ki determinations.


Cell Assay: Cell viability is assayed by the method using MTT. MTT-reactive cells are quantified at an absorbance of 570 nm using a micro-plate reader.

In VivoIn collagen-induced arthritis mice, FR180204 (100 mg/kg, i.p., b.i.d.) significantly decreases the severity of symptoms and body weight loss. In a mouse model of dengue virus (DENV) infection, FR180204 limits hepatocyte apoptosis, reduces DENV-induced liver injury, and improves Clinical parameters.
Animal modelCollagen-induced arthritis mouse model
Formulation & DosageSuspended in 0.1% methylcellulose solution; 100 mg/kg; i.p. injection
References

Naunyn Schmiedebergs Arch Pharmacol. 2007 Jan;374(4):311-6.