| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
Alaproclate hydrochloride targets the serotonin transporter (SERT) as a selective serotonin re-uptake inhibitor (SSRI). By inhibiting SERT, it increases the concentration of serotonin in the synaptic cleft. The compound also targets the NMDA receptor as a potent, reversible, and noncompetitive antagonist of the NMDA receptor coupled ion flow. This dual mechanism of action—SSRI activity combined with NMDA receptor antagonism—distinguishes Alaproclate from other SSRIs and makes it a valuable research tool.
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| ln Vitro |
In vitro studies demonstrate that Alaproclate hydrochloride is a selective and potent serotonin re-uptake inhibitor. It increases serotonin concentration in the synaptic cleft by inhibiting the serotonin transporter. The compound also acts as a potent, reversible, and noncompetitive antagonist of the NMDA receptor coupled ion flow. This dual mechanism makes it a valuable tool for studying the interplay between serotonergic and glutamatergic signaling in depression and anxiety. Detailed in vitro characterization data, including SERT inhibition and NMDA receptor antagonism, are available in the primary literature.
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| ln Vivo |
In vivo studies of Alaproclate hydrochloride have been conducted in the context of depression and anxiety research. As an orally active SSRI with additional NMDA receptor antagonist activity, it has been evaluated in animal models of depression and anxiety. The compound's dual mechanism may offer advantages over traditional SSRIs by providing faster onset of action or enhanced efficacy. Specific in vivo efficacy data in animal models are available in the primary literature. The compound was originally developed by Astra AB in the 1970s. Further research is ongoing to characterize its full therapeutic potential.
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| Enzyme Assay |
For serotonin transporter binding assays, membrane preparations from cells expressing recombinant SERT or from brain tissue are incubated with radiolabeled ligands (e.g., [3H]-citalopram or [3H]-paroxetine) and varying concentrations of Alaproclate hydrochloride. Non-specific binding is determined using excess unlabeled reference compounds. Following incubation at appropriate temperature (typically 4-25°C for 60-120 minutes), bound and free radioligands are separated by rapid filtration through glass fiber filters. Filters are washed and radioactivity counted by liquid scintillation. Ki values are calculated from competition curves. For NMDA receptor assays, receptor binding or ion flux is measured.
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| Cell Assay |
For in vitro cellular assays, cell lines expressing SERT or NMDA receptors are cultured in appropriate media under standard conditions (37°C, 5% CO2). Alaproclate hydrochloride is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. Serotonin uptake is measured by adding radiolabeled [3H]-5-HT and quantifying intracellular radioactivity. NMDA receptor activity is assessed by measuring ion flux or downstream signaling. Cell viability and cytotoxicity can be assessed using standard assays. Each concentration is tested in replicate wells with vehicle controls and positive controls.
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| Animal Protocol |
For in vivo animal studies, Alaproclate hydrochloride is typically formulated in suitable vehicles and administered via oral gavage due to its oral activity. Dosing regimens vary by study objective. For depression models (e.g., forced swim test, tail suspension test), animals are treated with compound and behavioral responses are recorded. For anxiety models (e.g., elevated plus maze, open field test), similar protocols are used. For pharmacokinetic studies, blood and brain tissue samples are collected at predetermined time points. All procedures must follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Alaproclate hydrochloride indicate it is orally active. The compound has a molecular weight of 292.20 and formula C13H19Cl2NO2. CAS number: 60719-83-7. Storage: typically at -20°C for powder; in solvent at -80°C. Solubility: soluble in DMSO and other organic solvents. As an SSRI, it is expected to have moderate oral bioavailability and good blood-brain barrier penetration. Specific pharmacokinetic parameters such as half-life, clearance, and bioavailability are reported in the primary literature.
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| Toxicity/Toxicokinetics |
According to available safety information, Alaproclate hydrochloride is intended for research purposes only. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. No clinical toxicity data are available.
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| References |
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| Additional Infomation |
Alaproclate hydrochloride (GEA 654 hydrochloride) is a selective and orally active SSRI that also acts as a potent, reversible, and noncompetitive antagonist of the NMDA receptor coupled ion flow. It was originally developed by Astra AB in the 1970s. It is used in research on depression and anxiety disorders. It has a molecular weight of 292.20 and formula C13H19Cl2NO2. It is for research use only with no regulatory approvals reported.
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| Molecular Formula |
C13H19CL2NO2
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|---|---|
| Molecular Weight |
292.20
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| Exact Mass |
291.079
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| CAS # |
60719-83-7
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| Related CAS # |
60719-82-6 (Parent); 57469-92-8 ( S isomer HCl); 66171-75-3 ( S isomer); 60719-83-7 (HCl)
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| PubChem CID |
11957454
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
324.8ºC at 760 mmHg
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| Flash Point |
150.2ºC
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| LogP |
4.053
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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 |
5
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| Heavy Atom Count |
18
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| Complexity |
260
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C(=O)OC(C)(C)CC1=CC=C(C=C1)Cl)N.Cl
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| InChi Key |
OPAKSOWFKIUFNP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H18ClNO2.ClH/c1-9(15)12(16)17-13(2,3)8-10-4-6-11(14)7-5-10;/h4-7,9H,8,15H2,1-3H3;1H
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| Chemical Name |
[1-(4-chlorophenyl)-2-methylpropan-2-yl] 2-aminopropanoate;hydrochloride
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| Synonyms |
Alaproclate hydrochloride; 60719-83-7; Alaproclate HCl; NIH506S9US; RefChem:110511;
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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 | 3.4223 mL | 17.1116 mL | 34.2231 mL | |
| 5 mM | 0.6845 mL | 3.4223 mL | 6.8446 mL | |
| 10 mM | 0.3422 mL | 1.7112 mL | 3.4223 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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