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| 50mg |
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| Targets |
cis-PDA acts as a non-specific antagonist of ionotropic glutamate receptors, including NMDA, AMPA, and kainate receptors. It blocks the responses mediated by these receptors, thereby inhibiting excitatory synaptic transmission. Additionally, cis-PDA acts as a partial agonist at NMDA receptors. This dual mechanism, acting as both an antagonist and a partial agonist, makes it a complex pharmacological tool for studying glutamatergic signaling. It has anticonvulsant activity.
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| ln Vitro |
cis-PDA demonstrates agonistic activity against the NMDA glutamate receptor with an effective dose of 10.0 μM when tested in a rat cortical slice preparation. As a general ionotropic receptor antagonist, it blocks NMDA, AMPA, and kainate-mediated responses. The compound's partial agonist activity at NMDA receptors suggests that it may have complex effects on glutamatergic neurotransmission, depending on the receptor subtype and experimental conditions.
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| ln Vivo |
In vivo, cis-PDA has been studied for its anticonvulsant activity. As a general ionotropic receptor antagonist, it can block excitatory synaptic transmission and may have neuroprotective effects in conditions of excitotoxicity. However, detailed in vivo efficacy data are limited, as the compound is primarily used as a research tool. Its partial agonist activity at NMDA receptors adds complexity to its in vivo effects.
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| Enzyme Assay |
In vitro assays for cis-PDA involve measuring its effects on ionotropic glutamate receptors using electrophysiological techniques. For NMDA receptor activity, Xenopus oocytes or HEK293 cells expressing recombinant NMDA receptors are used in two-electrode voltage-clamp or patch-clamp recordings. Receptors are activated by glutamate and glycine, and the effects of cis-PDA on current amplitude are measured. For AMPA and kainate receptors, similar protocols are used with appropriate agonists.
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| Cell Assay |
Cellular assays for cis-PDA are performed using cultured neurons or brain slices. In rat cortical slice preparations, the compound's effects on synaptic transmission are assessed by recording field excitatory postsynaptic potentials (fEPSPs) or population spikes. The compound is applied at concentrations ranging from 1 to 100 μM, and its effects on synaptic responses are measured. These assays are used to study the role of ionotropic glutamate receptors in synaptic transmission and plasticity.
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| Animal Protocol |
In vivo animal studies with cis-PDA are limited, as it is primarily a research tool. The compound has been studied for its anticonvulsant activity in animal models of epilepsy. Doses and routes of administration are not well documented. As a charged molecule, cis-PDA may have limited ability to cross the blood-brain barrier, necessitating direct administration into the central nervous system for in vivo studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for cis-PDA are limited, as it is a research compound not intended for therapeutic use. Its molecular weight is 173.17 g/mol. The compound is a polar, water-soluble dicarboxylic acid, which limits its ability to cross the blood-brain barrier. For in vivo studies, it is typically administered directly into the brain or cerebrospinal fluid.
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| Toxicity/Toxicokinetics |
Toxicological data for cis-PDA are limited. As an ionotropic glutamate receptor antagonist, the compound could potentially cause neurological effects by blocking excitatory neurotransmission. However, detailed toxicity studies have not been reported. The compound is intended for laboratory research only and should be handled with standard safety precautions.
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| References | |
| Additional Infomation |
See also: 2,3-piperidinedicarboxylic acid (note moved to).
cis-PDA is a research compound used as a pharmacological tool to study ionotropic glutamate receptor function. Its ability to block NMDA, AMPA, and kainate receptors, combined with its partial agonist activity at NMDA receptors, makes it a unique tool for investigating glutamatergic neurotransmission. The compound is not approved for clinical use and is intended for laboratory research only. |
| Molecular Formula |
C7H11NO4
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|---|---|
| Molecular Weight |
173.16
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| Exact Mass |
173.069
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| CAS # |
46026-75-9
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| PubChem CID |
11957663
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.363g/cm3
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| Boiling Point |
419.4ºC at 760mmHg
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| Flash Point |
207.5ºC
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| Index of Refraction |
1.52
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| LogP |
-2.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
12
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| Complexity |
204
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1C[C@H]([C@H](NC1)C(=O)O)C(=O)O
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| InChi Key |
PTLWNCBCBZZBJI-UHNVWZDZSA-N
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| InChi Code |
InChI=1S/C7H11NO4/c9-6(10)4-2-1-3-8-5(4)7(11)12/h4-5,8H,1-3H2,(H,9,10)(H,11,12)/t4-,5+/m1/s1
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| Chemical Name |
(2S,3R)-piperidine-2,3-dicarboxylic acid
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| Synonyms |
cisPDA; cis PDA; cis-PDA
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 | 5.7750 mL | 28.8750 mL | 57.7501 mL | |
| 5 mM | 1.1550 mL | 5.7750 mL | 11.5500 mL | |
| 10 mM | 0.5775 mL | 2.8875 mL | 5.7750 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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