| Size | Price | Stock | Qty |
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| 5g |
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| Other Sizes |
| Targets |
(R)-2-Amino-3-(3-(trifluoromethyl)phenyl)propanoic acid (TFMPA) is a potent and selective antagonist of the metabotropic glutamate receptor subtype 1 (mGluR1). This receptor is involved in various physiological and pathological processes in the central nervous system. By antagonizing mGluR1, TFMPA modulates glutamatergic signaling, which is implicated in neurological disorders such as Parkinson's disease, Alzheimer's disease, and epilepsy. As a phenylalanine analogue, it may also interact with other targets, but its primary reported mechanism is mGluR1 antagonism.
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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 activity of (R)-2-Amino-3-(3-(trifluoromethyl)phenyl)propanoic acid has been characterized as a potent and selective antagonist of the metabotropic glutamate receptor subtype 1 (mGluR1). In cell-based assays, it inhibits mGluR1-mediated signaling pathways, such as calcium mobilization. The compound's in vitro activity has been extensively studied in the context of neurological disorders, where it modulates glutamatergic transmission. As an amino acid derivative, it may also influence the secretion of anabolic hormones, although this is not its primary reported activity. |
| ln Vivo |
In vivo activity of (R)-2-Amino-3-(3-(trifluoromethyl)phenyl)propanoic acid has been investigated for its potential therapeutic applications in neurological disorders. Animal studies have explored its effects in models of Parkinson's disease, Alzheimer's disease, and epilepsy. As an mGluR1 antagonist, it is expected to modulate glutamatergic signaling in the central nervous system. However, detailed in vivo efficacy data from specific animal models are not extensively detailed in the available literature. Further research would be needed to fully characterize its in vivo pharmacological profile.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for (R)-2-Amino-3-(3-(trifluoromethyl)phenyl)propanoic acid would typically involve radioligand binding studies to assess its affinity for mGluR1. A common protocol involves incubating membrane preparations expressing mGluR1 with a radiolabeled mGluR1 ligand and varying concentrations of the test compound. The amount of bound radioligand is measured, and the IC50 value for displacement is determined. This assay directly measures the compound's ability to bind to the receptor. Functional assays, such as calcium mobilization assays in cells expressing mGluR1, can also be used to assess its antagonist activity.
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| Cell Assay |
Cell-based assays for (R)-2-Amino-3-(3-(trifluoromethyl)phenyl)propanoic acid would focus on its mGluR1 antagonist activity. For example, cells expressing mGluR1 could be treated with an mGluR1 agonist (e.g., glutamate) in the presence or absence of the compound, and downstream signaling pathways (e.g., calcium mobilization) could be measured. The ability of the compound to block agonist-induced signaling would demonstrate its functional antagonism. These assays are commonly used to evaluate the activity of mGluR1 modulators in drug discovery.
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| Animal Protocol |
In vivo animal experiments for (R)-2-Amino-3-(3-(trifluoromethyl)phenyl)propanoic acid would likely involve mouse or rat models of neurological disorders. For example, in a Parkinson's disease model, animals could be treated with the compound, and motor function or dopaminergic neuron survival could be assessed. In an epilepsy model, the compound's effect on seizure frequency or severity could be evaluated. These experiments would help determine the compound's therapeutic potential in vivo.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (R)-2-Amino-3-(3-(trifluoromethyl)phenyl)propanoic acid have not been fully characterized. As a small molecule (MW 233.19 g/mol), it is likely to be absorbed orally and cross the blood-brain barrier due to its lipophilic trifluoromethyl group. However, detailed ADME data, including half-life, bioavailability, and clearance, are not extensively available in the literature. The compound is typically stored as a powder at -20°C for up to 3 years or in solution at -80°C for up to 6 months. Further pharmacokinetic studies would be required to support its development as a therapeutic agent.
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| Toxicity/Toxicokinetics |
Toxicological data for (R)-2-Amino-3-(3-(trifluoromethyl)phenyl)propanoic acid is limited. As a research chemical, it is not intended for human use, and comprehensive toxicity studies have not been reported. The compound is generally considered safe for laboratory handling with standard precautions. The presence of a trifluoromethyl group may influence its toxicity profile. No specific information regarding acute toxicity, genotoxicity, or reproductive toxicity is available. Given its structural similarity to phenylalanine, it may have a low toxicity profile, but this has not been formally established.
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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):1793-1009.
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| Additional Infomation |
(R)-2-Amino-3-(3-(trifluoromethyl)phenyl)propanoic acid (TFMPA) is a synthetic amino acid derivative and a potent, selective mGluR1 antagonist. It has been extensively studied for its potential therapeutic applications in neurological disorders, including Parkinson's disease, Alzheimer's disease, and epilepsy. It is not a drug and has no approved therapeutic indications or clinical trial history. The compound is commercially available from various chemical suppliers for research purposes only. Its primary application is in medicinal chemistry and neuroscience research for studying mGluR1 function and developing new treatments for neurological disorders.
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| Molecular Formula |
C10H10F3NO2
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|---|---|
| Molecular Weight |
233.19
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| Exact Mass |
233.066
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| CAS # |
14464-67-6
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| PubChem CID |
7005132
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
301.2±42.0 °C at 760 mmHg
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| Flash Point |
135.9±27.9 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.502
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| LogP |
1.68
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
16
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| Complexity |
255
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC(=CC(=C1)C(F)(F)F)C[C@H](C(=O)O)N
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| InChi Key |
BURBNIPKSRJAIQ-MRVPVSSYSA-N
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| InChi Code |
InChI=1S/C10H10F3NO2/c11-10(12,13)7-3-1-2-6(4-7)5-8(14)9(15)16/h1-4,8H,5,14H2,(H,15,16)/t8-/m1/s1
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| Chemical Name |
(2R)-2-amino-3-[3-(trifluoromethyl)phenyl]propanoic 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) |
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 | 4.2883 mL | 21.4417 mL | 42.8835 mL | |
| 5 mM | 0.8577 mL | 4.2883 mL | 8.5767 mL | |
| 10 mM | 0.4288 mL | 2.1442 mL | 4.2883 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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