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Valproic acid
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Valproic acid图片
CAS NO:99-66-1
包装与价格:
包装价格(元)
500mg电议
1 g电议
5 g电议
25 g电议
50 g电议

产品名称
丙戊酸
VPA
2-Propylpentanoic Acid
产品介绍
Valproic acid (VPA) 是一种具有口服活性的HDAC抑制剂,IC50值为 0.5-2 mM,抑制HDAC1的活性,(IC50,400 μM),同时可诱导HDAC2的降解。Valproic acid 激活Notch1信号并抑制小细胞肺癌 (SCLC) 细胞的增殖。Valproic acid 可用于癫痫、双相情感障碍、代谢疾病、HIV 感染和偏头痛等的研究。
生物活性

Valproic acid (VPA) is an orally activeHDACinhibitor, withIC50in the range of 0.5 and 2 mM, also inhibitsHDAC1(IC50, 400 μM), and induces proteasomal degradation ofHDAC2. Valproic acid activatesNotch1signaling and inhibits proliferation in small cell lungcancer(SCLC) cells. Valproic acid is used in the treatment of epilepsy, bipolar disorder,metabolic disease, HIVinfectionand prevention of migraine headaches[1][2][3][4][5][6][7].

IC50& Target[5][6]

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[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].

Cell Viability Assay[1]

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 IC50of ~10 and 4 mM at 24 and 72 h.

Western Blot Analysis[1][2][5]

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[1]

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[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].

Animal Model:Female BALB/c nude mice, Kasumi-1 tumor model[3]
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[4]
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[5]
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.
分子量

144.21

性状

Liquid

Formula

C8H16O2

CAS 号

99-66-1

中文名称

丙戊酸;2-丙基戊酸;二丙基乙酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

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

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM6.9343 mL34.6717 mL69.3433 mL
5 mM1.3869 mL6.9343 mL13.8687 mL
10 mM0.6934 mL3.4672 mL6.9343 mL
*

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
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (693.43 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

  • 2.

    请依序添加每种溶剂: 0.5% CMC/saline water

    Solubility: 20 mg/mL (138.69 mM); Suspended solution; Need ultrasonic

  • 3.

    请依序添加每种溶剂: 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 ddH2O 中,得到澄清透明的生理盐水溶液
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin 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 μL20% 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.

    请依序添加每种溶剂: 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。

*以上所有助溶剂都可在本网站选购。