| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
Peripheral GABA_B receptors. L-Isovaline activates a long-lasting potassium conductance through its interaction with peripheral GABA_B receptors.
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|---|---|
| ln Vitro |
Commercial ergot supplements have been made from amino acids and their derivatives. They affect the release of anabolic hormones, the availability of fuel for activity, the ability to think clearly under pressure, and the prevention of muscular damage brought on by exertion. They are regarded as advantageous synergistic food ingredients [1].
L-Isovaline activates a long-lasting potassium conductance. It inhibits firing mainly by activating rectifying and possibly leak K⁺ currents. The compound suppresses rebound excitation in ventrobasal neurons, consistent with analgesic actions. It acts as an analgesic in mice by activating peripheral GABA_B receptors. |
| ln Vivo |
L-Isovaline acts as an analgesic in mice. It acts downstream to the cyclooxygenase system that NSAIDs inhibit, suggesting a means to avoid adverse effects such as gastrointestinal irritation. Its peripheral restriction (inability to cross the blood-brain barrier) makes it a peripherally acting analgesic without central nervous system side effects.
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| Enzyme Assay |
In vitro GABA_B receptor binding assays can be used to study the interaction of L-isovaline with peripheral GABA_B receptors. Radioligand binding studies using membranes from tissues expressing GABA_B receptors and radiolabeled GABA_B ligands (such as [³H]-baclofen) are conducted to determine binding affinity. Electrophysiological recordings from neurons can also be used to measure GABA_B receptor-mediated potassium currents.
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| Cell Assay |
In vitro cell-based assays for L-isovaline evaluate its effects on GABA_B receptor-mediated signaling. Cells expressing recombinant GABA_B receptors are loaded with calcium-sensitive dyes or used in electrophysiological patch-clamp recordings to measure the compound's ability to activate potassium conductances. The compound's effects on neuronal firing are assessed in primary neuronal cultures from peripheral ganglia.
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| Animal Protocol |
In vivo animal studies for L-isovaline typically use mouse models of pain. The compound is administered peripherally (e.g., intraperitoneally or locally) and analgesic efficacy is assessed using standard pain tests such as the tail-flick test, hot plate test, or formalin test. The lack of central nervous system penetration can be confirmed by measuring compound levels in brain tissue.
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| ADME/Pharmacokinetics |
L-Isovaline does not cross the blood-brain barrier. This peripheral restriction is a key feature of its pharmacological profile. Detailed pharmacokinetic parameters such as half-life, bioavailability, and metabolism are not extensively reported in the provided literature. The compound is a small amino acid with molecular weight approximately 117.15 g/mol.
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| Toxicity/Toxicokinetics |
Specific toxicity data for L-isovaline is not extensively reported. The compound acts downstream to the cyclooxygenase system that NSAIDs inhibit, suggesting it may avoid adverse effects such as gastrointestinal irritation. It is classified as a research-grade chemical and is not intended for human use.
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| References | |
| Additional Infomation |
See also: D-Isovaline (note moved to).
L-Isovaline (CAS# 595-40-4) is a non-proteinogenic amino acid that acts as an analgesic in mice by activating peripheral GABA_B receptors. It activates a long-lasting potassium conductance and inhibits neuronal firing. The compound does not cross the blood-brain barrier, making it peripherally restricted. It acts downstream to the cyclooxygenase system, potentially avoiding NSAID-like gastrointestinal side effects. It has not received FDA approval. |
| Molecular Formula |
C55H11NO2
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|---|---|
| Molecular Weight |
117.15
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| Exact Mass |
117.078
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| CAS # |
595-40-4
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| PubChem CID |
6971276
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
213.6±23.0 °C at 760 mmHg
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| Melting Point |
289.39°C (estimate)
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| Flash Point |
83.0±22.6 °C
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| Vapour Pressure |
0.1±0.9 mmHg at 25°C
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| Index of Refraction |
1.466
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| LogP |
0.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
8
|
| Complexity |
103
|
| Defined Atom Stereocenter Count |
1
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| SMILES |
CC[C@@](C)(C(=O)O)N
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| InChi Key |
GCHPUFAZSONQIV-YFKPBYRVSA-N
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| InChi Code |
InChI=1S/C5H11NO2/c1-3-5(2,6)4(7)8/h3,6H2,1-2H3,(H,7,8)/t5-/m0/s1
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| Chemical Name |
(2S)-2-amino-2-methylbutanoic acid
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| Synonyms |
NSC-1019; NSC 1019; Isovaline L-
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 8.5361 mL | 42.6803 mL | 85.3606 mL | |
| 5 mM | 1.7072 mL | 8.5361 mL | 17.0721 mL | |
| 10 mM | 0.8536 mL | 4.2680 mL | 8.5361 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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