| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| 10mg | |||
| Other Sizes |
| Targets |
Group II metabotropic glutamate receptors (mGlu2 and mGlu3). Highly selective agonist.
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|---|---|
| ln Vitro |
Acts as a selective agonist for group II mGluRs. Specific in vitro EC50 values for mGlu2 and mGlu3 are not detailed in standard references, but functional GTPgammaS assays confirm agonist activity. Inhibits glutamate release, influences cell proliferation via effects on D1 receptor-mediated motor responses, and reduces brain-derived neurotrophic factor (BDNF) levels.
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| ln Vivo |
In the dentate gyrus, 2R, 4R-APDC (1–10 nmol; ICV; once daily for 14 days) decreases cell growth [2].
In rats, (2R,4R)-APDC (1-10 nmol; intracerebroventricular, ICV; daily for 14 days) decreases cell proliferation in the dentate gyrus of adult rats. Specific anticonvulsant activity has been reported (e.g., in DBA/2 mice), though detailed efficacy data are not presented in standard references. Neuroprotective effects have been observed in models of hypoxia and brain injury. |
| Enzyme Assay |
Not applicable (functional agonist, not an enzyme inhibitor). For competitive binding: Group II mGluR radioligand binding assay. Membranes from cells expressing recombinant rat mGlu2/3 incubated with [3H]-LY341489 (a group II/III mGluR antagonist) and varying (2R,4R)-APDC concentrations. Ki values calculated from displacement curves; no specific IC50 values provided in standard references.
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| Cell Assay |
Functional GTPgammaS assays: Membranes from CHO cells expressing recombinant rat mGlu2 or mGlu3 incubated with [3⁵S]-GTPgammaS, GDP, and varying (2R,4R)-APDC concentrations. Agonist activity measured by increase in [3⁵S]-GTPgammaS binding (G-protein activation); EC50 values derived from concentration-response curves.
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| Animal Protocol |
Animal/Disease Models: Adult male SD (SD (Sprague-Dawley)) rat, body weight 300 to 350 g[2]
Doses: 1 nmol/10 μl; 10 nmol/10μl Route of Administration: ICV; one time/day for 14 days Experimental Results: Result in BrdU immunity in DG Reactive cells diminished. Rat cell proliferation model: Adult male Sprague-Dawley rats weighing 300-350g. (2R,4R)-APDC (1-10 nmol per injection) administered via intracerebroventricular (ICV) injection once daily for 14 days. Bromodeoxyuridine (BrdU, 50 mg/kg IP) injected 2 hours before sacrifice on day 14. Dentate gyrus cell proliferation measured by immunohistochemistry for BrdU-positive cells in hippocampal sections. Results: decreased cell proliferation at doses of 1-10 nmol. |
| ADME/Pharmacokinetics |
PK data specific to (2R,4R)-APDC are not detailed in standard references. As a charged amino acid derivative, systemic bioavailability is expected to be low, and ICV administration is commonly used to achieve CNS exposure. Distribution volume and half-life not reported.
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| Toxicity/Toxicokinetics |
Acute toxicity data: No data available for oral, inhalation, or dermal exposure. No data available for skin corrosion/irritation, serious eye damage/irritation, respiratory/skin sensitization, germ cell mutagenicity, carcinogenicity, or reproductive toxicity. As a research chemical, standard handling precautions should be followed to avoid skin/eye contact and ingestion. Aquatic toxicity unknown; minimal environmental release recommended.
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| References |
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| Additional Infomation |
(2R,4R)-4-aminopyrrolidine-2,4-dicarboxylic acid is a pyrrolidine dicarboxylic acid.
(2R,4R)-APDC is a highly selective, systemically-active (following ICV administration) agonist of group II mGluRs negatively coupled to adenylate cyclase. It has been shown to decrease cell proliferation in the dentate gyrus of adult rats, suggesting a role in adult neurogenesis. The compound has been studied in various CNS disease models including epilepsy, hypoxia-induced memory impairment, and traumatic brain injury. No clinical trials reported; serves as a standard research tool for group II mGluR pharmacology. The enantiomer (2S,4S)-APDC has different activity profiles, underscoring the importance of chirality. |
| Molecular Formula |
C₆H₁₀N₂O₄
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|---|---|
| Molecular Weight |
174.15
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| Exact Mass |
174.064
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| CAS # |
169209-63-6
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| PubChem CID |
5310984
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
-6.5
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
12
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| Complexity |
230
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| Defined Atom Stereocenter Count |
2
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| SMILES |
NC1(C(O)=O)CNC(C(O)=O)C1
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| InChi Key |
XZFMJVJDSYRWDQ-AWFVSMACSA-N
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| InChi Code |
InChI=1S/C6H10N2O4/c7-6(5(11)12)1-3(4(9)10)8-2-6/h3,8H,1-2,7H2,(H,9,10)(H,11,12)/t3-,6-/m1/s1
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| Chemical Name |
(2R,4R)-4-aminopyrrolidine-2,4-dicarboxylic acid
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| Synonyms |
(2R,4R)APDC; (2R,4R) APDC
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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 | 5.7422 mL | 28.7109 mL | 57.4218 mL | |
| 5 mM | 1.1484 mL | 5.7422 mL | 11.4844 mL | |
| 10 mM | 0.5742 mL | 2.8711 mL | 5.7422 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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