| Size | Price | Stock | Qty |
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| 5g |
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| Other Sizes |
| Targets |
L-4FPG targets the neutral amino acid transporters ASCT1 (SLC1A4) and ASCT2 (SLC1A5). These transporters are responsible for the sodium-dependent transport of neutral amino acids across cell membranes. By inhibiting these transporters, L-4FPG can modulate amino acid availability in cells, which may affect various physiological processes. Its ability to cross the blood-brain barrier and reduce amphetamine-induced hyperlocomotion suggests it may also interact with central nervous system targets.
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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].
In vitro, L-4FPG is an inhibitor of ASCT1 and ASCT2. Its activity is confirmed through transport assays measuring the uptake of radiolabeled amino acids in cells expressing these transporters. Detailed IC₅₀ values for transporter inhibition are not extensively reported in the available literature. Its good brain penetration is a key feature for its activity in the central nervous system. |
| ln Vivo |
In vivo, L-4FPG shows good brain penetration and potently reduces amphetamine-induced hyperlocomotion. This suggests it has central nervous system activity, potentially through the modulation of amino acid levels or neurotransmitter systems. These in vivo activities make it a valuable research tool for studying neurological disorders.
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| Enzyme Assay |
Non-cell-based assays for L-4FPG are not typical, as its mechanism involves the inhibition of membrane transporters. However, its binding to ASCT1 and ASCT2 can be studied using membrane preparations from cells expressing these transporters and radiolabeled substrates. Its ability to cross the blood-brain barrier can be assessed using in vitro models of the BBB.
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| Cell Assay |
Cellular assays for L-4FPG are performed using cells expressing ASCT1 or ASCT2. Cells are treated with the compound, and the uptake of radiolabeled amino acids is measured. The compound's ability to inhibit amino acid transport is quantified. Its effects on cell function and signaling can also be assessed.
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| Animal Protocol |
In vivo animal models for L-4FPG include models of amphetamine-induced hyperlocomotion to assess its central nervous system effects. The compound is administered via appropriate routes, and locomotor activity is measured. Its brain penetration is confirmed by measuring its concentration in brain tissue.
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| ADME/Pharmacokinetics |
L-4FPG has a molecular weight of 155.15 g/mol and a molecular formula of C₈H₈FNO₂. Its CAS number is 19883-57-9. The compound is supplied as a solid with a purity of ≥98%. It is soluble in DMSO. Storage conditions: -20°C for 3 years; in solvent: -80°C for 1 year. The compound is a glycine derivative. Detailed pharmacokinetic parameters such as half-life and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for L-4FPG are not extensively reported in the available literature. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
[1]. Luckose F, et al. Effects of amino acid derivatives on physical, mental, and physiological activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
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| Additional Infomation |
L-4FPG is also known as (S)-4-Fluorophenylglycine. It is a non-proteinogenic, fluorinated aromatic amino acid derivative and a glycine analog. L-4FPG inhibits the neutral amino acid transporters ASCT1 and ASCT2. It shows good brain penetration and potently reduces amphetamine-induced hyperlocomotion. Its CAS number is 19883-57-9.
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| Molecular Formula |
C8H8FNO2
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|---|---|
| Molecular Weight |
169.16
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| Exact Mass |
169.053
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| CAS # |
19883-57-9
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| PubChem CID |
853015
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
289.9±30.0 °C at 760 mmHg
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| Melting Point |
300ºC
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| Flash Point |
129.1±24.6 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.565
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| LogP |
0.99
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
12
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| Complexity |
166
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC1C([H])=C([H])C(=C([H])C=1[H])[C@@]([H])(C(=O)O[H])N([H])[H]
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| InChi Key |
JKFYKCYQEWQPTM-ZETCQYMHSA-N
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| InChi Code |
InChI=1S/C8H8FNO2/c9-6-3-1-5(2-4-6)7(10)8(11)12/h1-4,7H,10H2,(H,11,12)/t7-/m0/s1
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| Chemical Name |
(2S)-2-amino-2-(4-fluorophenyl)acetic acid
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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) |
H2O : ~1.96 mg/mL (~11.59 mM )
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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 | 5.9116 mL | 29.5578 mL | 59.1156 mL | |
| 5 mM | 1.1823 mL | 5.9116 mL | 11.8231 mL | |
| 10 mM | 0.5912 mL | 2.9558 mL | 5.9116 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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