| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| Targets |
cis-ABCD acts as a potent, competitive, and selective inhibitor of the high-affinity, Na+-dependent plasma membrane glutamate transporter (EAAT). It inhibits glutamate uptake, thereby increasing extracellular glutamate levels. Additionally, cis-ABCD binds to NMDA receptors with high affinity (Ki = 0.052 μM) and acts as an agonist at this receptor. It is selective for NMDA over kainate and AMPA receptors. This dual mechanism makes it a valuable tool for studying glutamatergic neurotransmission.
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| ln Vitro |
cis-ABCD is a potent and selective inhibitor of glutamate uptake, acting as a linear competitive inhibitor of D-[3H]aspartate uptake. It has been shown to inhibit the high-affinity, Na+-dependent plasma membrane glutamate transporter with high potency. As an NMDA receptor agonist, it binds to NMDA receptors with a Ki of 0.052 μM. It demonstrates no significant activity at kainate or AMPA receptors (Kis >300 μM).
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| ln Vivo |
In vivo, cis-ABCD has been studied for its effects on glutamatergic neurotransmission. As a glutamate uptake inhibitor, it increases extracellular glutamate levels, which may have excitotoxic effects. As an NMDA receptor agonist, it can activate NMDA receptors and modulate synaptic plasticity. However, detailed in vivo efficacy data are limited, as the compound is primarily used as a research tool to study glutamate transporter function and NMDA receptor pharmacology.
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| Enzyme Assay |
In vitro assays for cis-ABCD involve measuring the inhibition of glutamate uptake or the binding to NMDA receptors. For glutamate uptake inhibition, synaptosomes or cells expressing EAAT transporters are incubated with [3H]-glutamate or D-[3H]aspartate in the presence of varying concentrations of cis-ABCD. Uptake is terminated by filtration, and radioactivity is measured by scintillation counting. IC50 values are calculated from inhibition curves. For NMDA receptor binding, radioligand binding assays are performed using [3H]-MK-801 or other NMDA-selective ligands.
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| Cell Assay |
Cellular assays for cis-ABCD are performed using cultured neurons or cells expressing recombinant glutamate transporters or NMDA receptors. Glutamate uptake is measured by incubating cells with [3H]-glutamate in the presence or absence of cis-ABCD. For NMDA receptor activation, calcium imaging using fluorescent indicators such as Fura-2 or Fluo-4 is used to measure intracellular calcium levels in response to glutamate and glycine application in the presence of cis-ABCD.
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| Animal Protocol |
In vivo animal studies with cis-ABCD are limited, as the compound is primarily used as a research tool in vitro. When used in vivo, it is typically administered via intracerebral injection to study the effects of glutamate transporter inhibition or NMDA receptor activation on synaptic transmission, behavior, or neurodegeneration. Doses and routes of administration vary depending on the experimental design. Detailed protocols are not widely available.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for cis-ABCD are limited, as it is a research compound not intended for therapeutic use. Its molecular weight is 159.14 g/mol. The compound is a polar, water-soluble amino acid derivative, which limits its ability to cross the blood-brain barrier. For in vivo studies, it is typically administered directly into the brain via intracerebroventricular or intraparenchymal injection.
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| Toxicity/Toxicokinetics |
Toxicological data for cis-ABCD are limited. As a glutamate uptake inhibitor and NMDA receptor agonist, the compound has the potential to cause excitotoxicity by increasing extracellular glutamate levels and overactivating NMDA receptors. This should be considered when designing experiments. The compound is intended for laboratory research only and should be handled with standard safety precautions.
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| References |
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| Additional Infomation |
cis-ABCD is a research compound used as a pharmacological tool to study glutamate transporter function and NMDA receptor pharmacology. It is a potent inhibitor of glutamate uptake and a high-affinity NMDA receptor agonist. The compound's dual mechanism makes it valuable for studying glutamatergic neurotransmission and excitotoxicity. It is not approved for clinical use and is intended for laboratory research only.
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| Molecular Formula |
C6H9NO4
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|---|---|
| Molecular Weight |
159.14
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| Exact Mass |
159.053
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| CAS # |
73550-55-7
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| Related CAS # |
trans-ACBD;117488-23-0
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| PubChem CID |
1214
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.568g/cm3
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| Boiling Point |
288.1ºC at 760 mmHg
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| Flash Point |
128ºC
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| Index of Refraction |
1.587
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| LogP |
-3.5
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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 |
11
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| Complexity |
207
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N[C@@]1(C[C@@H](C1)C(O)=O)C(O)=O
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| InChi Key |
GGMYWPBNZXRMME-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H9NO4/c7-6(5(10)11)1-3(2-6)4(8)9/h3H,1-2,7H2,(H,8,9)(H,10,11)
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| Chemical Name |
1-aminocyclobutane-1,3-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 | 6.2838 mL | 31.4189 mL | 62.8378 mL | |
| 5 mM | 1.2568 mL | 6.2838 mL | 12.5676 mL | |
| 10 mM | 0.6284 mL | 3.1419 mL | 6.2838 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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