[CAS NO. 1069-66-5]  Valproic acid sodium

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PRODUCTS SPECIFICATIONS [1069-66-5]

Catalog
HY-10585A
Brand
MCE
CAS
1069-66-5

DESCRIPTION [1069-66-5]

Overview

MDLMFCD00078604
Molecular Weight166.19
Molecular FormulaC8H15NaO2
SMILESO=C(O[Na])C(CCC)CCC

For research use only. We do not sell to patients.


Summary

Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC 50 in the range of 0.5 and 2 mM, also inhibits HDAC1 ( IC 50 , 400 μM), and induces proteasomal degradation of HDAC2 . Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium 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] .


IC50 & Target

HDAC1

400 μM (IC 50 )

HDAC

0.5-2 mM (IC 50 )

HDAC2

Autophagy

Mitophagy


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] .

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

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 IC 50 of ~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: 24 h (HeLa); 0-18 h (Neuro2A); 0-24 h (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.

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] .

MCE 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 [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.

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT02872428 Dr. Hasan Alam|University of Michigan
Shock,Hemorrhagic|Trauma
November 2016 Phase 1
NCT02068586 Sidney Kimmel Cancer Center at Thomas Jefferson University|Pfizer|Thomas Jefferson University
Ciliary Body and Choroid Melanoma, Medium+Large Size|Ciliary Body and Choroid Melanoma, Small Size|Iris Melanoma|Stage I Intraocular Melanoma|Stage IIA Intraocular Melanoma|Stage IIB Intraocular Melanoma|Stage IIIA Intraocular Melanoma|Stage IIIB Intraocular Melanoma|Stage IIIC Intraocular Melanoma
November 19, 2014 Phase 2
NCT04310176 National Cancer Institute, Naples
Ras-mutated Metastatic Colorectal Cancer
May 24, 2019 Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)


Solvent & Solubility

In Vitro:

H 2 O : 125 mg/mL ( 752.15 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 6.0172 mL 30.0860 mL 60.1721 mL
5 mM 1.2034 mL 6.0172 mL 12.0344 mL
10 mM 0.6017 mL 3.0086 mL 6.0172 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

    Solubility: 100 mg/mL (601.72 mM); Clear solution; Need ultrasonic

* All of the co-solvents are available by MCE.


Synonyms

Pentanoic acid, 2-propyl-, sodium salt (1:1)
Valeric acid, 2-propyl-, sodium salt
Pentanoic acid, 2-propyl-, sodium salt
Sodium dipropylacetate
Sodium α,α-dipropylacetate
Sodium bispropylacetate
Sodium valproate
Dipropylacetate sodium
Valproate sodium
Sodium 2-propylpentanoate
Epilim
Sodium 2-propylvalerate
Convulex
Orfiril
Valerin
KW 6066N
Depakene
Acediprol
Depakene syrup 8
Depakin
Depacon
Depakine chronosphere
Selenica R
Depakene R
Valpron
Vupral
Micropakine LP
Valproic acid sodium salt
VPA
Encorate