Valproic acid.|99-66-1|(丙戊酸; Dipropylacetic Acid)-陌孚医药/Medlife

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Valproic acid. (Synonyms: 丙戊酸; Dipropylacetic Acid)

目录号: PC10335 纯度: ≥98%

CAS No. :99-66-1

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PC10335-10mM (in 1mL DMSO)	10mM(in1mLDMSO)	¥780.00	请登录

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中文名称

Valproic acid.

中文别名

丙戊酸;二丙基乙酸;2-丙基戊酸;2,2-二-正丙基乙酸;2-Propylvaleric Acid 2-丙基戊酸;2-正丙基正戊酸;丙戊酸 EP标准品;丙戊酸 USP标准品;丙戊酸标准品;丙戊酸系统适应性 EP标准品;托美汀钠二水合物标准品;2,2-二正丙基乙酸;A-丙基戊酸;α-丙基戊酸

英文名称

2-Propylpentanoic acid

英文别名

2-Propylpentanoic acid;Dipropylacetic acid;2,2-Di-n-propylacetic acid;2-Propylvaleric Acid;Valproic acid;Valproic acid solution;[14C]-Valproic acid;[3H]-Valproic acid;2,2-BIS(TRIFLUOROMETHYL)PROPIONIC ACID;2-propyl-pentanoic acid;Convulex;Depakene;Depakine;di-n-propyl-acetic acid;Ergenyl;Mylproin;sodium valproate;Valproate;VPA

Cas No.

99-66-1

分子式

C₈H₁₆O₂

分子量

144.21

包装储存

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Valproic acid (VPA) 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 activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.

性状

Liquid

IC50 & Target[1][2]

HDAC1

400 μM (IC₅₀)

HDAC

0.5-2 mM (IC₅₀)

HDAC2

Autophagy

Mitophagy

体外研究(In Vitro)

Valproic acid (VPA) (0-15 mM; 24 and 72 h) inhibits Hela cell growth in a dose- and time- dependent manner.
Valproic acid (10 mM; 24 h) significantly attenuates the activities of total, cytosol and nuclear HDACs.
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.
Valproic acid (0-20 mM; 24 h) activates Tcf/Lef-dependent transcription and synergizes with lithium.
Valproic acid (0-5 mM; 0-18 h) increases β-catenin levels in Neuro2A cells.
Valproic acid (0-2 mM; 0-24 h) stimulates phosphorylation of AMPK and ACC in hepatocytes.
Valproic acid (0-10 mM; 2 days) induces Notch1 signaling and morphologic differentiation, suppresses production of NE tumor markers in SCLC cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	HeLa cells
Concentration:	0, 1, 3, 5, 10 and 15 mM
Incubation Time:	24 and 72 h
Result:	HeLa cell growth was dose- and time-dependently decreased with an IC₅₀ of ~10 and 4 mM at 24 and 72 h.

Western Blot Analysis

Cell Line:	HeLa cells, Neuro2A cells or primary mouse hepatocytes
Concentration:	10 mM (HeLa); 0, 2, and 5 mM (Neuro2A); 0.2, 0.4, 0.8, 1.2 and 2 mM (hepatocytes)
Incubation Time:	10 mM (HeLa); 0, 2, and 5 mM (Neuro2A); 0.2, 0.4, 0.8, 1.2 and 2 Mm (hepatocytes)
Result:	Increased the form of acetylated histone 3. Reduced PARP, induced cleavage PARP, and downregulated Bcl-2. Increased β-catenin levels. Increased the phosphorylation of AMPK and ACC.

Cell Cycle Analysis

Cell Line:	HeLa cells
Concentration:	0, 1, 3, 5, 10 and 15 mM
Incubation Time:	24 h
Result:	Induced a G1 phase arrest at 1–3 mM, significantly induced a G2/M phase arrest at 10 mM, and increased the percentage of sub-G1 cells in HeLa cells in a dose-dependent manner at 24 h.

体内研究(In Vivo)

Valproic acid (VPA) (500 mg/kg; i.p.; daily for 12 days) inhibits tumor angiogenesis in mice transplanted with Kasumi-1 cells.
Valproic acid (350 mg/kg; i.p.; once) enhances social behavior in rats.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c nude mice, Kasumi-1 tumor model
Dosage:	500 mg/kg
Administration:	Intraperitoneal injection, daily for 12 days
Result:	Inhibited tumor growth and tumor angiogenesis. Inhibited the mRNA and protein expression of VEGF, VEGFR2 and bFGF. Inhibited HDAC activity and increased acetylation of histone H3. Enhanced the accumulation of hyperacetylated histone H3 on VEGF promoters.

Animal Model:	Timed-pregnant Long Evans rats
Dosage:	350 mg/kg
Administration:	Intraperitoneal injection, once
Result:	Demonstrated more social investigation and play fighting than control animals.

Animal Model:	Obese phenotype of ob/ob mice
Dosage:	0.26% (w/v)
Administration:	Oral via drinking water, 14 days
Result:	Revealed a marked reduction in the accumulation of fats in the liver as compared with the untreated mice, significantly decreased liver mass to body mass, decreased serum triglyceride concentrations, and did not induce hepatotoxicity.

运输条件

Room temperature or refrigerated transportation.

储存方式

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[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. [Information]

[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. [Information]

[3]. Zhang ZH, et al. Valproic acid inhibits tumor angiogenesis in mice transplanted with Kasumi 1 leukemia cells. Mol Med Rep. 2013 Nov 28. [Information]

[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. [Information]

[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. [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (693.43 mM; Need ultrasonic)

H₂O : 1 mg/mL (6.93 mM; Need ultrasonic and warming)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	6.9343 mL	34.6717 mL	69.3433 mL
5 mM	1.3869 mL	6.9343 mL	13.8687 mL
10 mM	0.6934 mL	3.4672 mL	6.9343 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (693.43 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

建议依照次序添加每种溶剂： 0.5% CMC/saline water
Solubility: 20 mg/mL (138.69 mM); Suspended solution; Need ultrasonic
3.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (17.34 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (17.34 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
4.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (17.34 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (17.34 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
5.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (17.34 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (17.34 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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