| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg |
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| Targets |
(S)-3,4-DCPG targets metabotropic glutamate receptor 8a (mGluR8a), a G protein-coupled receptor that is a member of the group III metabotropic glutamate receptors. mGluR8a is predominantly expressed in the brain, including in the hippocampus, cortex, and basal ganglia, where it plays a role in synaptic transmission, plasticity, and neuroprotection. By selectively activating mGluR8a, (S)-3,4-DCPG modulates glutamate signaling, reducing excitotoxicity and providing neuroprotection. The compound's potent and selective agonism of mGluR8a makes it a valuable tool for studying mGluR8a function and for developing therapies for neurological disorders, including Parkinson's disease, epilepsy, and anxiety. Its EC50 of 31 nM demonstrates its high potency.
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| ln Vitro |
In vitro, (S)-3,4-DCPG acts as a selective agonist of mGluR8a with an EC50 of 31 nM in AV12-664 cells expressing human mGluR8a. The compound shows high selectivity for mGluR8a over other metabotropic glutamate receptors. In cell-based assays, (S)-3,4-DCPG activates mGluR8a-mediated signaling pathways, including inhibition of adenylyl cyclase and modulation of ion channels. The compound's activity is concentration-dependent, with effective concentrations ranging from 1 nM to 10 µM. Its potent and selective agonism makes it a valuable tool for studying mGluR8a function and for developing novel therapeutics for neurological disorders. Detailed mechanistic studies are needed to fully characterize its effects on mGluR8a signaling and neuronal function.
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| ln Vivo |
In vivo, (S)-3,4-DCPG has been studied in animal models of Parkinson's disease. The compound reverses motor deficits in prolonged, but not acute, models of Parkinson's disease. This suggests that mGluR8a activation may provide neuroprotective effects that require prolonged treatment to become apparent. The compound is typically administered via intraperitoneal injection in preclinical studies. Its ability to reverse motor deficits in Parkinson's disease models makes it a promising candidate for further development as a neuroprotective therapy. However, detailed pharmacokinetic profiles and comprehensive toxicology data are limited. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro mGluR8a activation assay for (S)-3,4-DCPG typically uses cells expressing recombinant human mGluR8a (e.g., AV12-664 cells). The assay is performed in 96-well or 384-well plates with cells loaded with a calcium-sensitive fluorescent dye (e.g., Fluo-4) or using a cAMP assay. Cells are stimulated with varying concentrations of the test compound (typically 0.1 nM to 10 µM), and calcium influx or cAMP levels are measured using a fluorescence plate reader or HTRF-based detection. EC50 values are calculated from dose-response curves using nonlinear regression. For selectivity profiling, the compound is tested against other metabotropic glutamate receptors. Positive controls (e.g., known mGluR8a agonists) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, neuronal cell lines or primary neurons expressing mGluR8a are treated with (S)-3,4-DCPG at concentrations ranging from 0.1 nM to 10 µM for 1-24 hours. Intracellular calcium levels are measured using fluorescent calcium indicators. cAMP levels are measured using ELISA or HTRF-based detection. Neuronal excitability is assessed by electrophysiological recordings. Neuroprotective effects are assessed by treating cells with the compound and exposing them to neurotoxic insults (e.g., glutamate, oxidative stress), followed by cell viability assays. For mechanism studies, the effects of the compound on mGluR8a signaling pathways are investigated by Western blotting. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo Parkinson's disease studies, rodent models (e.g., 6-OHDA-lesioned rats or MPTP-treated mice) are used. (S)-3,4-DCPG is administered via intraperitoneal injection at doses ranging from 0.1 to 10 mg/kg, typically daily for 1-4 weeks. Motor function is assessed using behavioral tests such as the rotarod test, open field test, and apomorphine-induced rotation test. Neuroprotection is assessed by measuring dopamine levels in the striatum and by immunohistochemical analysis of tyrosine hydroxylase-positive neurons. At study endpoint, brain tissues are harvested for biochemical analysis. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of (S)-3,4-DCPG have been partially characterized. The compound has a molecular weight of 239.18 and is water-soluble (25-100 mg/ml). Following intraperitoneal or oral administration, the compound shows moderate absorption with a Tmax of 0.5-1 hour. Plasma half-life is estimated to be 1-2 hours. The compound distributes into tissues including brain, consistent with its central nervous system activity. Plasma protein binding is moderate. Metabolism is primarily hepatic, with conjugation as a major pathway. The compound is eliminated primarily via renal excretion. Oral bioavailability is limited due to first-pass metabolism. The compound's ability to penetrate the blood-brain barrier supports its CNS applications. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of (S)-3,4-DCPG are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 10 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
(S)-3,4-DCPG is a selective mGluR8a agonist with an EC50 of 31 nM. It reverses motor deficits in prolonged Parkinson's disease models. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥98%) for laboratory use only. Its potent and selective mGluR8a agonism makes it a valuable tool for studying mGluR8a function, glutamate signaling, and for developing neuroprotective therapies for Parkinson's disease and other neurological disorders.
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| Molecular Formula |
C10H9NO6
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| Molecular Weight |
239.18156
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| Exact Mass |
239.043
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| CAS # |
201730-11-2
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| PubChem CID |
16062593
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| Appearance |
White to off-white solid powder
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| LogP |
0.867
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
342
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC(=C(C=C1[C@@H](C(=O)O)N)C(=O)O)C(=O)O
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| InChi Key |
IJVMOGKBEVRBPP-ZETCQYMHSA-N
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| InChi Code |
InChI=1S/C10H9NO6/c11-7(10(16)17)4-1-2-5(8(12)13)6(3-4)9(14)15/h1-3,7H,11H2,(H,12,13)(H,14,15)(H,16,17)/t7-/m0/s1
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| Chemical Name |
4-[(S)-amino(carboxy)methyl]phthalic 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 | 4.1810 mL | 20.9048 mL | 41.8095 mL | |
| 5 mM | 0.8362 mL | 4.1810 mL | 8.3619 mL | |
| 10 mM | 0.4181 mL | 2.0905 mL | 4.1810 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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