Valproic acid sodium salt (Sodium valproate)

Valproic acid is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.

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In DMSO USD 420 In stock
USD 97 In stock
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Valproic acid sodium salt (Sodium valproate) Chemical Structure

Valproic acid sodium salt (Sodium valproate) Chemical Structure
Molecular Weight: 166.19

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Valproic acid sodium salt (Sodium valproate) is available in the following compound libraries:

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Product Description

Biological Activity

Description Valproic acid is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
In vitro Valproic acid acts through a distinct pathway that involves direct inhibition of histone deacetylase (IC(50) for HDAC1 = 0.4 mM). Valproic acid mimics the histone deacetylase inhibitor trichostatin A, causing hyperacetylation of histones in cultured cells. Valproic acid, like trichostatin A, also activates transcription from diverse exogenous and endogenous promoters. Valproic acid and trichostatin A have remarkably similar teratogenic effects in vertebrate embryos, while non-teratogenic analogues of valproic acid do not inhibit histone deacetylase and do not activate transcription. [1] Valproic acid induces proliferation of peroxisomes in the rodent liver. Valproic acid at a concentration of 1 mM induces relief of this repression by Gal4 fusions of N‐CoR, TR or PPARδ in a cell line expressing the ligand‐binding domain of PPARδ fused to the DNA‐binding domain of the glucocorticoid receptor (GR) together with a GR‐controlled reporter gene. Valproic acid induces accumulation of hyperacetylated histone and inhibits HDAC activity. Valproic acid induces a specific type of differentiation characterized by reduced proliferation, morphological alterations, marker gene expression and particularly the accumulation of the AP-2 transcription factor as a potential marker of neuronal or neural crest cell-like differentiation in F9 teratocarcinoma cells. Valproic acid impairs cell proliferation or survival as indicated by decreased incorporation of [3H]thymidine in F9 and P19 teratocarcinoma cells. [2]
In vivo Valproic acid delays growth of the primary tumors in the MT‐450 rat breast cancer model. [2]
Features

Protocol(Only for Reference)

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Phiel CJ, et al. J Biol Chem, 2001, 276(39), 36734-36741.

[2] Göttlicher M, et al. EMBO J, 2001, 20(24), 6969-6978.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-09-13)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02011750 Enrolling by invitation Toxoplasmosis|Schizophrenia University of Pittsburgh|Mansoura University|Stanley Medical Research Institute March 2013 Phase 4
NCT01791868 Not yet recruiting Generalized Convulsive Status Epilepticus|Intensive Care Unit Assistance Publique - Hôpitaux de Paris February 2013 --
NCT01730313 Not yet recruiting Nodding Syndrome Centers for Disease Control and Prevention|Ministry of Health, Uganda February 2013 Phase 2
NCT01619644 Active, not recruiting Rubinstein-Taybi Syndrome University Hospital, Bordeaux|Fondation Syndrome de Rubinstein-Taybi April 2012 Phase 2
NCT00713622 Completed Epilepsy Eisai Inc.|Eisai Limited June 2008 Phase 4

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Chemical Information

Download Valproic acid sodium salt (Sodium valproate) SDF
Molecular Weight (MW) 166.19
Formula

C8H15NaO2

CAS No. 1069-66-5
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 33 mg/mL (198 mM)
Water 33 mg/mL (198 mM)
Ethanol 33 mg/mL (198 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name sodium 2-propylpentanoate

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Customer Reviews (1)


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Rating
Source Dr. Zhang of Tianjin Medical University. Valproic acid sodium salt (Sodium valproate) purchased from Selleck
Method Western blot
Cell Lines
Concentrations 0-10 μM
Incubation Time
Results Increased Histone acetylation in cells treated with Sodium valproate was observed.

Product Citations (1)

Tech Support & FAQs

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