| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
CGP 78608 targets the glycine-binding site of the N-methyl-D-aspartate (NMDA) receptor. It is a potent and selective antagonist with an IC50 of 5-6 nM. It displays > 500-fold selectivity over kainate and AMPA receptors (IC50 = 2.7 and 3 μM, respectively). It also potentiates GluN1/GluN3A-mediated glycine currents with an EC50 of 26.3 nM.
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| ln Vitro |
GluN1/GluN3A receptors' glycine sensitivity is decreased by CGP-78608 hydrochloride via intersubunit allosteric interactions between GluN1 and GluN3A agonist binding domain (ABD) sites [2]. One of the causes of ammonia neurotoxicity, ammonia-dependent cGMP production, is reduced or eliminated by CGP 78608 hydrochloride [3].
In vitro, CGP 78608 is a potent NMDA receptor antagonist at the glycine site (IC50 = 5-6 nM). It shows high selectivity (>500-fold) over kainate and AMPA receptors. It acts as a potentiator of GluN1/GluN3A-mediated glycine currents (EC50 = 26.3 nM). It exhibits anticonvulsant activity. |
| ln Vivo |
CGP-78608 hydrochloride intraperitoneally injected mice demonstrated effective anticonvulsant effects in the electric shock-induced convulsions test [1].
In vivo, CGP 78608 has anticonvulsant activity. Its ability to antagonize the glycine site of the NMDA receptor makes it a valuable tool for studying the role of NMDA receptors in neurological disorders, such as epilepsy and excitotoxicity. |
| Enzyme Assay |
Non-cellular assays for CGP 78608 involve measuring its binding affinity to the NMDA receptor glycine site. This is done using radioligand binding assays with membranes prepared from brain tissue or cells expressing recombinant receptors. A radiolabeled glycine site antagonist is used, and the compound's ability to displace it is measured.
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| Cell Assay |
In vitro cellular assays for CGP 78608 are conducted in cells expressing NMDA receptors. Its antagonistic activity is assessed by measuring NMDA receptor-mediated currents using electrophysiological techniques (patch-clamp) in the presence of glycine and the compound. Its potentiating effect on GluN1/GluN3A-mediated currents can also be studied.
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| Animal Protocol |
In vivo animal experiments with CGP 78608 are conducted in models of seizures and epilepsy. The compound is administered, and its ability to prevent or reduce seizure activity is assessed. Its effects on other neurological conditions can be studied in appropriate models.
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| ADME/Pharmacokinetics |
CGP 78608 has a molecular weight of 263.63 (free base). It is soluble in water and DMSO. It is typically stored as a powder at -20°C. Its pharmacokinetic properties, such as brain penetration and half-life, would need to be characterized for in vivo use.
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| Toxicity/Toxicokinetics |
CGP 78608 is considered to have low toxicity based on its use as a research compound. However, comprehensive toxicological data are not extensively published. The compound is intended for research use only and is not approved for human therapeutic use.
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| References | |
| Additional Infomation |
CGP 78608 hydrochloride is the monohydrochloride salt of CGP 78608. It is a potent and selective NMDA receptor antagonist that acts on the glycine binding site (IC50 = 5 nM). Its selectivity for phycocyanin and AMPA receptors is more than 500 times higher than that for CGP 78608 (IC50 values of 2.7 μM and 3 μM, respectively). It exhibits anticonvulsant activity in vivo after systemic administration. It can be used as a prodrug, NMDA receptor antagonist, and anticonvulsant. It is the conjugate base of CGP 78608(1+).
CGP 78608 hydrochloride is a potent and selective antagonist at the glycine-binding site of the NMDA receptor (IC50 = 5-6 nM). It displays >500-fold selectivity over kainate and AMPA receptors and has anticonvulsant activity. It also potentiates GluN1/GluN3A-mediated glycine currents. |
| Molecular Formula |
C11H14BRCLN3O5P
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|---|---|
| Molecular Weight |
414.576721668243
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| Exact Mass |
412.954
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| CAS # |
1135278-54-4
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| PubChem CID |
24978530
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
485
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| Defined Atom Stereocenter Count |
1
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| SMILES |
BrC1C=C2C(=C(C=1)CN[C@H](C)P(=O)(O)O)NC(C(N2)=O)=O.Cl
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| InChi Key |
MZQQZBPMRPDKTB-JEDNCBNOSA-N
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| InChi Code |
InChI=1S/C11H13BrN3O5P.ClH/c1-5(21(18,19)20)13-4-6-2-7(12)3-8-9(6)15-11(17)10(16)14-8;/h2-3,5,13H,4H2,1H3,(H,14,16)(H,15,17)(H2,18,19,20);1H/t5-;/m0./s1
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| Chemical Name |
[(1S)-1-[(7-bromo-2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methylamino]ethyl]phosphonic acid;hydrochloride
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| Synonyms |
CGP 78608 HCl; CGP 78608 HCl
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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 | 2.4121 mL | 12.0604 mL | 24.1208 mL | |
| 5 mM | 0.4824 mL | 2.4121 mL | 4.8242 mL | |
| 10 mM | 0.2412 mL | 1.2060 mL | 2.4121 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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