| 名稱 | Valproic acid sodium salt |
| 描述 | Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt 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. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect. |
| 細(xì)胞實(shí)驗(yàn) | 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 The plates are additionally incubated for 3 h at 37°C. Medium is withdrawn from the plates by pipetting and 200 mL DMSO is added to each well to solubilize the formazan crystals.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. |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 在MT-450大鼠乳腺癌模型中,Valproic acid對(duì)原發(fā)腫瘤的生長(zhǎng)具有延遲作用. |
| 體內(nèi)活性 | 在培養(yǎng)的細(xì)胞中,Valproic acid與組蛋白去乙酰化酶抑制劑曲古抑菌素A一樣可引起組蛋白去乙?；alproic acid,如曲古抑菌素 A,也激活不同的外源性和內(nèi)源性啟動(dòng)子的轉(zhuǎn)錄。在脊椎動(dòng)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(duì)HDAC1的IC50為0.4 mM。在F9和P19畸胎瘤細(xì)胞中,Valproic acid抑制細(xì)胞增殖或存活,表現(xiàn)為[3H]胸苷滲入下降。Valproic acid還促進(jìn)嚙齒動(dòng)物肝臟過氧化物酶體增殖。在表達(dá)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(bào)告基因融合的細(xì)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)乙酰化組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(biāo)志是增殖減少,形態(tài)改變,AP-2的轉(zhuǎn)錄因子累積和標(biāo)志物基因表達(dá),AP-2是神經(jīng)元或神經(jīng)嵴細(xì)胞樣分化的F9畸胎瘤細(xì)胞的潛在標(biāo)記物。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (300.84 mM)
H2O : 16.6 mg/mL (100 mM)
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| 關(guān)鍵字 | bipolar disorder | Valproic acid | anticonvulsant | Valproic acid sodium salt | SCLC | Mitophagy | hepatic fat accumulation | degradation | Histone deacetylases | HIV | HDAC | Mitochondrial Autophagy | Notch | inhibit | Apoptosis | anticancer | Endogenous Metabolite | headaches | epilepsy | small cell lung cancer | Inhibitor | Human immunodeficiency virus | proteasomal | Notch1 | Valproic acid sodium | migraine | Autophagy |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Emtricitabine | Hydroxychloroquine | Lamivudine | Stavudine | Paeonol | Sodium 4-phenylbutyrate |
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