| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
PPDA targets NMDA receptors, with preferential binding to GluN2C/GluN2D-containing receptors. Ki values are 0.096 μM for GluN2C, 0.125 μM for GluN2D, 0.31 μM for GluN2B, and 0.55 μM for GluN2A subunits. This selectivity profile makes it a valuable tool for distinguishing between NMDA receptor subtypes. The compound is an enantiomer with 2S,3R-configuration.
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| ln Vitro |
In vitro activity data for PPDA demonstrate its subtype-selective NMDA receptor antagonism. The compound’s Ki values of 0.096 μM for GluN2C, 0.125 μM for GluN2D, 0.31 μM for GluN2B, and 0.55 μM for GluN2A confirm its preferential binding to GluN2C/GluN2D-containing receptors. This selectivity is approximately 5- to 6-fold higher for GluN2C/GluN2D compared to GluN2A-containing receptors.
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| ln Vivo |
In vivo activity data for PPDA are not extensively detailed in the available literature. The compound is primarily used as a research tool for studying NMDA receptor subunit-specific functions in neurological and psychiatric disorders. Its receptor binding profile suggests potential for in vivo studies investigating the roles of GluN2C and GluN2D subunits in synaptic transmission, plasticity, and neuroprotection.
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| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for PPDA involve radioligand binding displacement assays using membranes expressing recombinant NMDA receptor subunits. Ki values are determined by measuring the ability of PPDA to displace a radiolabeled ligand from GluN2A, GluN2B, GluN2C, and GluN2D subunit-containing receptors. Binding affinity is calculated using standard competitive binding equations.
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| Cell Assay |
In vitro cell-based assays for PPDA are not extensively documented. The compound is primarily characterized through receptor binding assays rather than cell-based functional assays. Functional antagonism can be assessed using electrophysiological recordings in cells expressing specific NMDA receptor subunit combinations, measuring the compound’s ability to inhibit NMDA-evoked currents.
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| Animal Protocol |
In vivo animal studies for PPDA are not detailed in the available literature. As a subtype-selective NMDA receptor antagonist, typical in vivo evaluation would involve administration to animal models of neurological or psychiatric disorders to assess the functional roles of GluN2C/GluN2D-containing receptors. Behavioral, electrophysiological, and neurochemical endpoints would be monitored.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of PPDA are not extensively reported. The compound has a molecular weight of 378.38 g/mol, a molecular formula of C21H18N2O5, and a purity of ≥98% (HPLC). It is soluble in 2 eq. NaOH at 18.92 mg/mL (50 mM) and in DMSO at 37.84 mg/mL (100 mM). Storage: at +4°C. The compound is provided as a solid powder.
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| Toxicity/Toxicokinetics |
Specific toxicological data for PPDA are not detailed in the available literature. The compound is classified for laboratory research use only and is not intended for human therapeutic use. As an NMDA receptor antagonist, potential toxicities would relate to effects on glutamatergic neurotransmission, though formal toxicological profiles are not reported.
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| References | |
| Additional Infomation |
(2S,3R)-PPDA is a 1-(phenanthrene-2-ylcarbonyl)piperazine-2,3-dicarboxylic acid with a 2S,3R configuration. It is an NMDA receptor antagonist. It is the enantiomer of (2R,3S)-PPDA.
PPDA (CAS 684283-16-7) is a subtype-selective NMDA receptor antagonist that preferentially binds to GluN2C/GluN2D-containing receptors. Ki values are 0.096 μM for GluN2C, 0.125 μM for GluN2D, 0.31 μM for GluN2B, and 0.55 μM for GluN2A. The compound is sold under license from UNeMed Corporation. No clinical trial or approved indication data are available. |
| Molecular Formula |
C21H18N2O5
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|---|---|
| Molecular Weight |
378.378025531769
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| Exact Mass |
756.243
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| CAS # |
684283-16-7
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| PubChem CID |
20811874
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
0.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
638
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| Defined Atom Stereocenter Count |
2
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| SMILES |
OC([C@@H]1[C@H](C(=O)O)NCCN1C(C1C=CC2C3C=CC=CC=3C=CC=2C=1)=O)=O
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| InChi Key |
IWWXIZOMXGOTPP-MSOLQXFVSA-N
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| InChi Code |
InChI=1S/C21H18N2O5/c24-19(23-10-9-22-17(20(25)26)18(23)21(27)28)14-7-8-16-13(11-14)6-5-12-3-1-2-4-15(12)16/h1-8,11,17-18,22H,9-10H2,(H,25,26)(H,27,28)/t17-,18+/m1/s1
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| Chemical Name |
(2S,3R)-1-(phenanthrene-2-carbonyl)piperazine-2,3-dicarboxylic 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 | 2.6428 mL | 13.2142 mL | 26.4285 mL | |
| 5 mM | 0.5286 mL | 2.6428 mL | 5.2857 mL | |
| 10 mM | 0.2643 mL | 1.3214 mL | 2.6428 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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