Valproic acid sodium salt
作者：齊岳
發(fā)布時間：2023-09-11
09:25:21
點擊數(shù)：
產(chǎn)品名稱：Valproic acid sodium salt
產(chǎn)品描述：
| 產(chǎn)品描述 | Valproate Sodium is the sodium salt form of valproic acid with anti-epileptic activity. Valproate sodium is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, valproate sodium increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproate sodium may also affect potassium channels, thereby creating a direct membrane-stabilizing effect. |
| 靶點活性 | histone deacetylase 1 (HDAC1):0.4 mM |
| 體外活性 | 在0大鼠乳腺*模型中,Valproic acid對原發(fā)的生長具有延遲作用. |
| 體內(nèi)活性 | 在培養(yǎng)的細胞中,Valproic acid與組蛋白去乙?；敢种苿┣乓志谹一樣可引起組蛋白去乙酰化。Valproic acid,如曲古抑菌素 A,也激活不同的外源性和內(nèi)源性啟動子的轉(zhuǎn)錄。在脊椎動物的胚胎中,Valproic acid和曲古抑菌素A的致畸作用非常相似,卻不激活轉(zhuǎn)錄。 通過不同的途徑Valproic acid可直接抑制組蛋白脫乙?；?對HDAC1的IC50為0.4 mM。在F9和P19畸胎瘤細胞中,Valproic acid抑制細胞增殖或存活,表現(xiàn)為[3H]胸苷滲入下降。Valproic acid還促進嚙齒動物肝臟過氧化物酶體增殖。在表達糖皮質(zhì)激素受體的DNA結(jié)合域和PPARδ的配體結(jié)合結(jié)構(gòu)域,以及GR控制的報告基因融合的細胞中,Valproic acid（1 mM）抑制與N-COR,TR或PPARδ融合的Gal4釋放。Valproic acid誘導(dǎo)乙?；M蛋白積累的減少并抑制HDAC活性。Valproic acid誘導(dǎo)特定類型分化,標志是增殖減少,形態(tài)改變,AP-2的轉(zhuǎn)錄因子累積和標志物基因表達,AP-2是神經(jīng)元或神經(jīng)嵴細胞樣分化的F9畸胎瘤細胞的潛在標記物。 |
| 激酶實驗 | The activity of caspase-3, -8 and -9 is assessed using the caspase-3, -8 and -9 colorimetric assay kits, respectively. In brief, 1×106?cells in a 60-mm culture dish are incubated with 10 mM Valproic acid for 24 h. The cells are then washed in PBS and suspended in 5 volumes of lysis buffer provided with the kit. Protein concentrations are determined using the Bradford method. Supernatants containing 50 μg total protein are used to determine caspase-3, -8 and -9 activities. The supernatants are added to each well in 96-well microtiter plates with DEVD-pNA, IETD-pNA or LEHD-pNA as caspase-3, -8 and -9 substrates and the plates are incubated at 37°C for 1 h. The optical density of each well is measured at 405 nm using a microplate reader. The activity of caspase-3, -8 and -9 is expressed in arbitrary absorbance units. |
| 細胞實驗 | Valproic acid is dissolved in DMSO. In brief, 5×105?cells are seeded in 96-well microtiter plates for MTT assays. After exposure to the designated doses of Valproic acid for the indicated times, MTT solution [20 mL: 2 mg/mL in phosphate-buffered saline (PBS)] is added to each well of the 96-well plates. The plates are additionally incubated for 3 h at 37°C. Medium is withdrawn from the plates by pipetting and 200 mL DMSO is added to each well to solubilize the formazan crystals. The optical density is measured at 570 nm using a microplate reader. |
| 別名 | 丙戊酸鈉, Sodium Valproate |
| 分子量 | 166.2 |
| 分子式 | C8H15NaO2 |
| CAS No. | 1069-66-5 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 8.3 mg/mL (50 mM)
H2O: 16.6 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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