| 中文名称: | CID755673 | ||||
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| 英文名称: | CID755673 | ||||
| 别名: | CID755673 7-Hydroxy-2,3,4,5-tetrahydro-1H-benzofuro[2,3-c]azepin-1-one | ||||
| CAS No: | 521937-07-5 | 分子式: | C12H11NO3 | 分子量: | 217.22 |
| CAS No: | 521937-07-5 | ||||
| 分子式: | C12H11NO3 | ||||
| 分子量: | 217.22 | ||||
基本信息
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产品编号：C10865 |
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产品名称：CID755673 |
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CAS: |
521937-07-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
217.22 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
43mg/mL (197.95mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内（现配现用） |
2%DMSO+30%peg300+2%t-80+ddaH2O |
6mg/mL |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
4.6036mL |
23.0181mL |
46.0363mL |
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5mM |
0.9207mL |
4.6036mL |
9.2073mL |
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10mM |
0.4604mL |
2.3018mL |
4.6036mL |
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50mM |
0.0921mL |
0.4604mL |
0.9207mL |
生物活性
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产品描述 |
是高效选择性的PKD1抑制剂，IC50 of 值为182nM。 |
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靶点/IC50 |
PKD1 182nM (IC50) |
PKD3 227nM (IC50) |
PKD2 280nM (IC50) |
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体外研究 |
CID755673 blocks phorbol ester-induced endogenous PKD1 activation in LNCaP cells in a concentration-dependent manner.CID755673 inhibits the known biological actions of PKD1 including phorbol ester-induced class IIa histone deacetylase 5 nuclear exclusion, vesicular stomatitis virus glycoprotein transport from the Golgi to the plasma membrane, and the ilimaquinone-induced Golgi fragmentation. CID755673 inhibits prostate cancer cell proliferation,cell migration, and invasion. |
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体内研究 |
Acute administration of the PKD inhibitor CID755673 to normal mice reduces both PKD1 and 2 phosphorylation in a time and dose-dependent manner. Chronic CID755673 administration to T2D db/db mice for two weeks reduces expression of the gene expression signature of PKD activation, enhances indices of both diastolic and systolic left ventricular function and is associated with reduced heart weight. |
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推荐实验方法(仅供参考)
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激酶实验： |
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The radiometric kinase assay is carried out by coincubating 0.5μCi of [γ-32P]ATP, 20μMATP,50ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKIIα proteins, and 2.5μg of Syntide-2 in 50μL of kinase buffer that contains 50mM Tris-HCl, pH 7.5, 4mM MgCl2, 10mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range. |
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细胞实验: |
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The wound-induced migration is triggered by scraping the cells with a plastic pipette tip, and the wound is imaged immediately. The DU145 cells are then are treated with or without CID755673 at different concentrations. The wound is imaged immediately (0 h) and at different intervals with an inverted phase-contrast microscope with a ×10 objective. At the end of the assay, cells are fixed with methanol and stained with crystal violet for a final image. |
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动物实验: |
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Mice: For acute inhibitor studies, C57BL6 mice are administered a single dose of vehicle (5% DMSO in PBS, pH 7.4), or the selective PKD inhibitor CID755673 at 1 or 10mg/kg body weight.Mice are killed one or four hr later and heart collected for later analysis. For chronic inhibitor experiments, 8-week old db/db mice receives vehicle or CID755673 at 1 or 10mg/kg bodyweight for 16 days, by daily intraperitoneal (i.p.) injection. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
