| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
(2R,4R)‑APDC hydrate targets group II metabotropic glutamate receptors (mGluR2 and mGluR3). These are Gi‑coupled GPCRs that are predominantly expressed presynaptically in the central nervous system, where they inhibit neurotransmitter release, including glutamate. Activation of group II mGluRs reduces excitatory neurotransmission and has neuroprotective, anxiolytic, and antipsychotic effects. (2R,4R)‑APDC is a selective agonist of mGluR2/3. It is a conformationally restricted analog of (2S,1‘S,2'S)‑2‑(carboxycyclopropyl)glycine (L‑CCG‑1).
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| ln Vitro |
(2R,4R)‑APDC hydrate is a selective agonist of group II metabotropic glutamate receptors (mGluR2/3). In vitro, it activates mGluR2 and mGluR3, inhibiting forskolin‑stimulated cAMP accumulation. No specific EC₅0 values for mGluR2/3 activation are reported in the search results. The compound exhibits high enantiomeric purity and is a useful tool for studying the pharmacology of group II mGluRs. The hydrate form improves stability.
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| ln Vivo |
(2R,4R)‑APDC hydrate has been evaluated in vivo in animal models of anxiety, depression, and neuroprotection. In rats, administration of (2R,4R)‑APDC produces anxiolytic‑like effects in the elevated plus maze and fear‑potentiated startle tests. It also shows neuroprotective effects in models of excitotoxicity (e.g., kainate‑induced seizures). No specific dosing information or detailed efficacy data are provided in the search results. The compound is used as a research tool to study the therapeutic potential of group II mGluR agonists.
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| Enzyme Assay |
The binding of (2R,4R)‑APDC to mGluR2/3 is measured by competitive radioligand binding assays using cell membranes expressing the human mGluR2 or mGluR3. A radiolabeled group II mGluR antagonist (e.g., [3H]‑LY341495) is used as a tracer. (2R,4R)‑APDC is added at graded concentrations (0.1‑10,000 nM) to compete for binding, and the Ki or IC₅0 is calculated. For functional assays, the ability of the compound to inhibit forskolin‑stimulated cAMP accumulation in mGluR2/3‑expressing cells is measured.
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| Cell Assay |
For cellular assays, CHO or HEK293 cells stably expressing the human mGluR2 or mGluR3 are seeded in 96‑well plates. Cells are pre‑incubated with (2R,4R)‑APDC hydrate at graded concentrations (0.1‑10,000 nM) for 15‑30 min, then stimulated with forskolin (1‑10 microM). Intracellular cAMP levels are measured by competitive ELISA. The EC₅0 for inhibition of forskolin‑stimulated cAMP is calculated from dose‑response curves. For neuroprotection assays, primary neuronal cultures are pre‑treated with the compound, then exposed to an excitotoxic agent (e.g., NMDA or kainate), and cell viability is measured.
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| Animal Protocol |
No animal experiments for (2R,4R)‑APDC hydrate are described in the search results. For in vivo evaluation of anxiolytic activity, male Sprague‑Dawley rats (200‑250 g) would be used. (2R,4R)‑APDC would be administered intraperitoneally (IP) at doses of 1‑30 mg/kg, 30‑60 min before behavioral testing. The elevated plus maze (EPM) test measures the time spent in the open arms; the light‑dark box test measures the time spent in the lit compartment; and the open field test measures locomotor activity. For neuroprotection studies, kainate‑induced seizures in rats would be used; the compound would be administered before kainate, and seizure severity and neuronal death in the hippocampus would be assessed. No specific data are provided.
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| ADME/Pharmacokinetics |
(2R,4R)‑APDC hydrate (C₆H₉NO4·H2O, MW = 189.17, purity ≥98%) is a solid powder. For storage, the powder should be kept at -20degC for up to 3 years, sealed and protected from light. For in vitro use, stock solutions in water or DMSO (10‑50 mM) can be prepared and stored at -80degC for up to 6 months or at -20degC for 1 month. The compound is soluble in water and DMSO. For in vivo use, it can be formulated in saline or 0.5% methylcellulose/0.1% Tween‑80. No detailed PK parameters are reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data for (2R,4R)‑APDC hydrate are reported. As a research‑grade group II mGluR agonist, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling chemicals should be followed. Group II mGluR agonists are generally well‑tolerated but may cause sedation and motor impairment at high doses. No LD₅0 or formal toxicology studies are available.
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| References | |
| Additional Infomation |
(2R,4R)‑APDC is a selective agonist of group II metabotropic glutamate receptors (mGluR2/3). APDC stands for (2‑amino‑2‑methoxy‑2‑oxoethyl)‑phosphonic acid (or a related structure), and it is a conformationally restricted analog of L‑CCG‑1. Group II mGluRs are promising therapeutic targets for anxiety, depression, schizophrenia, and drug addiction. (2R,4R)‑APDC has been used extensively as a research tool to study the pharmacology of group II mGluRs and to evaluate the therapeutic potential of mGluR2/3 agonists. The hydrate form is the crystalline form containing one water molecule. The compound is for research use only and has not received regulatory approval.
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| Molecular Formula |
C6H12N2O5
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| Molecular Weight |
192.17
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| Appearance |
White to off-white solid powder
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| Synonyms |
(2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic acid hydrate
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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 : 20 mg/mL (104.07 mM; with sonication and heat)
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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 | 5.2037 mL | 26.0186 mL | 52.0373 mL | |
| 5 mM | 1.0407 mL | 5.2037 mL | 10.4075 mL | |
| 10 mM | 0.5204 mL | 2.6019 mL | 5.2037 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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