| CAS |
No.76584-70-8 |
| 英文名称 |
Divalproex Sodium |
| 别名 |
双丙戊酸钠;Valproate semisodium;Epival; |
| 分子式 |
C16H31NaO4 |
| 分子量 |
310.41 |
| 溶解性 |
Soluble in Water/DMSO ≥5mg/mL |
| 纯度 |
≥98% |
| 外观(性状) |
Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD00879852 |
| SMILES |
CCCC(CCC)C(=O)O.CCCC(CCC)C(=O)[O-].[Na+] |
| InChIKey |
MSRILKIQRXUYCT-UHFFFAOYSA-M |
| InChI |
InChI=1S/2C8H16O2.Na/c2*1-3-5-7(6-4-2)8(9)10;/h2*7H，3-6H2，1-2H3，(H，9，10);/q;;+1/p-1 |
| PubChem CID |
23663956 |
| 靶点 |
HDAC |
| 通路 |
DNA Damage/DNA Repair;Epigenetics;NF-κB |
| 背景说明 |
Divalproex Sodium是一种HDAC抑制剂。 |
| 生物活性 |
Valproic acid (VPA) sodium (2:1) is an orally active HDAC inhibitor， with IC50 in the range of 0.5 and 2 mM， also inhibits HDAC1 (IC50， 400 μM)， and induces proteasomal degradation of HDAC2. Valproic acid sodium (2:1) activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium (2:1) is used in the treatment of epilepsy， bipolar disorder， metabolic disease， HIV infection and prevention of migraine headaches[1][2][3][4][5][6][7]. |
| In Vitro |
Valproic acid (VPA) (0-15 mM; 24 and 72 h) inhibits Hela cell growth in a dose- and time- dependent manner[1].Valproic acid (10 mM; 24 h) significantly attenuates the activities of total， cytosol and nuclear HDACs[1].Valproic acid (0-15 mM; 24 h) induces a G1 phase arrest at 1–3 mM and a G2/M phase arrest at 10 mM， and increases the percentage of sub-G1 cells in HeLa cells. Valproic acid also induces necrosis， apoptosis and lactate dehydrogenase (LDH) release[1].Valproic acid (0-20 mM; 24 h) activates Tcf/Lef-dependent transcription and synergizes with lithium[2].Valproic acid (0-5 mM; 0-18 h) increases β-catenin levels in Neuro2A cells[2].Valproic acid (0-2 mM; 0-24 h) stimulates phosphorylation of AMPK and ACC in hepatocytes[5].Valproic acid (0-10 mM; 2 days) induces Notch1 signaling and morphologic differentiation， suppresses production of NE tumor markers in SCLC cells[6]. |
| In Vivo |
Valproic acid (VPA) (500 mg/kg; i.p.; daily for 12 days) inhibits tumor angiogenesis in mice transplanted with Kasumi-1 cells[3].Valproic acid (350 mg/kg; i.p.; once) enhances social behavior in rats[4].Valproic acid (0.26% (w/v); p.o. via drinking water; 14 days) decreases liver mass， hepatic fat accumulation， and serum glucose in obese mice without hepatotoxicity[5]. |
| 数据来源文献 |
[1]. Han BR， et al. Valproic acid inhibits the growth of HeLa cervical cancer cells via caspase-dependent apoptosis. Oncol Rep. 2013 Dec;30(6):2999-3005.
[2]. Valproic acid， et al. Histone deacetylase is a direct target of valproic acid， a potent anticonvulsant， mood stabilizer， and teratogen. J Biol Chem. 2001 Sep 28;276(39):36734-41.
[3]. Zhang ZH， et al. Valproic acid inhibits tumor angiogenesis in mice transplanted with Kasumi 1 leukemia cells. Mol Med Rep. 2013 Nov 28.
[4]. Cohen OS， et al. Acute prenatal exposure to a moderate dose of valproic acid increases social behavior and alters gene expression in rats. Int J Dev Neurosci. 2013 Dec;31(8):740-50.
[5]. Avery LB， et al. Valproic Acid Is a Novel Activator of AMP-Activated Protein Kinase and Decreases Liver Mass， Hepatic Fat Accumulation， and Serum Glucose in Obese Mice. Mol Pharmacol. 2014 Jan;85(1):1-10.
[6]. Platta CS， et al. Valproic acid induces Notch1 signaling in small cell lung cancer cells. J Surg Res. 2008 Jul;148(1):31-7.
[7]. Routy JP， et al. Valproic acid in association with highly active antiretroviral therapy for reducing systemic HIV-1 reservoirs: results from a multicentre randomized clinical study. HIV Med. 2012 May;13(5):291-6. |
| 规格 |
10mg |
| 单位 |
瓶 |
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