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FRAX486
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产品编号 | 包装单位 | 单价(元) | 国内现货 | 国外库存 | 询价单 |
4086730 | 5 MG | 1111 | |||
4086730 | 25 MG | 3890 |
产品别名
1232030-35-1
FRAX486
6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
FRAX 486
FRAX-486
6-(2,4-Dichlorophenyl)-8-ethyl-2-(3-fluoro-4-(piperazin-1-yl)phenylamino)pyrido[2,3-d] pyrimidin-7(8H)-one
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C25H23Cl2FN6O |
Molecular weight | 513.39 |
MDL number | MFCD26793866 |
NACRES | NA.77 |
Biochem/physiol Actions【生化/生理作用】 | FRAX486 is a potent, group I-selective p21-activated kinase (PAK) inhibitor (PAK1/2/3 IC50 = 8.25/39.5/55.3 nM; group II PAK4 IC50 = 779 nM). FRAX486 effectively inhibits PAK-mediated PKD1 Ser203 phosphorylation and PAK1/2 Ser144/141 autophosphorylation upon angiotensin II (ANGII) stimulation of rat IEC-18 cells (IC50 ∼0.5 μM) and exhibits in vivo efficacy in rescuing the autism-like phenotypes among Fmr1 knockout fragile syndrome (FXS) mice (20 mg/kg s.c.) as well as in ameliorating schizophrenia-associated dendritic spine deterioration among Disc1 knockdown mice (10 μg/g or 10 mg/kg i.p.) with good pharmacokinetic properties and blood–brain barrier (BBB) permeability. |
产品性质
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | powder |
color【颜色】 | white to beige |
solubility【溶解性】 | DMSO: 2 mg/mL, clear |
storage temp.【储存温度】 | −20℃ |
SMILES string | FC1=CC(NC2=NC(N3CC)=C(C=N2)C=C(C4=CC=C(C=C4Cl)Cl)C3=O)=CC=C1N5CCNCC5 |
安全信息
Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
WGK | WGK 3 |