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Home › Products › Ion Channels › Ligand-Gated Ion Channels › GABA(A) Receptors › Agonists

Certificate of Analysis

  • Bioassay Tested
    The specificity of this antibody has been validated in a knockout (KO) or knockdown (KD) system.

Valerenic acid

(-)-Valerenic Acid, (2E)-3-[(4S,7R,7aR)-3,7-dimethyl-2,4,5,6,7,7a-hexahydro-1H-inden-4-yl]-2-methylacrylic acid

A Positive Allosteric Modulator of the GABAA Receptors

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Overview

Cat #: V-140
Alternative Name (-)-Valerenic Acid, (2E)-3-[(4S,7R,7aR)-3,7-dimethyl-2,4,5,6,7,7a-hexahydro-1H-inden-4-yl]-2-methylacrylic acid
Lyophilized Powder yes
Source Synthetic
MW: 234.33
Purity: >98% (HPLC)
Form Lyophilized Powder
Effective concentration 10 - 200 µM
Chemical name (2E)-3-[(4S,7R,7aR)-2,4,5,6,7,7a-Hexadydro-3,7-dimethyl-1H-inden-4-yl]-2-methyl-2-propenoic acid
Molecular formula C15H22O2
CAS No.: 3569-10-6
PubChem CID 6440940
Activity Valerenic acid is a positive allosteric modulator of GABAA receptors that displays preference for β2 or β3 subunit receptors. Directly activates the receptor and also blocks the channel at high concentrations. Displays an anxiolytic and sedative activity in vivo1-3. Also acts as a partial agonist of 5-HT5A receptors4.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility Soluble in Ethanol and DMSO.
Up to 200 mM in DMSO. Centrifuge all product preparations before use (5,000 x g for 1 min).
Storage of solutions Up to four weeks at 4°C or three months at -20°C.
Scientific background

Valerenic acid was first isolated in 1957 from the rhizome and roots of valerian (Valeriana offi-cinalis). Valerian is one of the oldest medicinal herbs in folk medicine and has been used for various afflictions like insomnia, anxiety, and pain. Valerenic acid was found to be pharmacologically active monoterpene acting through binding to the GABAA receptor1.

Valerenic acid acts as an anti-inflammatory agent by inhibiting the transcription of NF-κB, one essential transcription factor controlling the expression of numerous inflammation-related genes. In addition, evidence suggests that Valerenic acid acts as an agonist for 5-HT receptors (serotonin receptors), which are G-coupled receptors that mediates neuronal activity via regulating cyclic adenosine monophosphate (cAMP) levels2.

In-vivo studies that conducted on xenograft glioblastoma multiforme (GBM) mice models shown that Valerenic acid induce cell death of GBM cells by inducing AMPK activation. Therefore, Valerenic acid may serve as a potential anti-tumor agent towards GBM patients3.

Target GABAA receptor
Lyophilized Powder
For research purposes only, not for human use
Last Update: 02/01/2024

Specifications

Citations

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Applications

Scientific Background

Related Products

Antibodies

  1. Anti-GABA(A) α1 Receptor (extracellular) Antibody (#AGA-001)
  2. Anti-GABA(A) α1 Receptor (extracellular)-ATTO Fluor-488 Antibody (#AGA-001-AG)
  3. Anti-GABA(A) β1 Receptor Antibody (#AGA-010)
  4. Anti-GABA(A) β3 Receptor Antibody (#AGA-013)
  5. Guinea pig Anti-GABA(A) α1 Receptor (extracellular) Antibody (#AGA-001-GP (formerly AGP-083))

Pharmacological tools

Blockers/Antagonists: peptides/peptide toxins
  1. α-Bungarotoxin (#B-100)
Blockers/Antagonists: small molecules
  1. (+)-Bicuculline (#B-135)
  2. (-)-Bicuculline methiodide (#B-136)
  3. (-)-Bicuculline methochloride (#B-137)
  4. Bilobalide (#B-145)
  5. Etbicyphat (#E-175)
  6. GABA(A)-Compound 1b (#CMG-004)
  7. Gabazine hydrobromide (#G-216)
  8. Oroxylin A (#O-160)
  9. Picrotoxin (#P-325)
  10. Tracazolate hydrochloride (#T-230)
  11. U 93631 (#U-120)
  12. α-Asarone (#A-260)
Activators/Agonists: small molecules
  1. CGS 20625 (#C-390)
  2. Isoguvacine hydrochloride (#I-185)
  3. γ-Aminobutyric acid (#G-110)
Modulators: peptides/peptide toxins
  1. MmTx1 Toxin (#STM-550)
  2. MmTx1 Toxin-ATTO Fluor-488 (#STM-550-AG)
  3. MmTx2 Toxin (#STM-600)
  4. Waglerin-1 (#STW-001)
  5. α-Bungarotoxin-ATTO Fluor-488 (#B-100-AG)
  6. α-Bungarotoxin-ATTO Fluor-633 (#B-100-FR)
  7. α-Bungarotoxin-Biotin (#B-100-B)
  8. α-Bungarotoxin-FITC (#B-100-F)
Modulators: small molecules
  1. 2'MeO6MF (#M-245)
  2. AA 29504 (#A-370)
  3. Amentoflavone (#A-165)
  4. Chlormethiazole hydrochloride (#C-360)
  5. Ganaxolone (#G-120)
  6. SJM-3 (#S-215)
  7. Tracazolate hydrochloride (#T-230)

Explorer kits & Research packs

Explorer kits
  1. GABA(A) α Receptor Antibody Explorer Kit (#AK-228)
  2. GABA(A) Receptor Agonist Explorer Kit (#EK-425)
  3. GABA(A) Receptor Antagonist Explorer Kit (#EK-420)
  4. GABA(A) Receptor Antibody Explorer Kit (#AK-229)
  5. GABA(A) Receptor Modulator Explorer Kit (#EK-360)
Research packs
  1. GABA(A) α1 Receptor Basic Research Pack (#ESB-800)
  2. GABA(A) α1 Receptor Deluxe Research Pack (#ESD-800)
  3. GABA(A) α1 Receptor Premium Research Pack (#ESP-800)

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