1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR
  3. CGP 78608 hydrochloride

CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 hydrochloride acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). Anticonvulsant activity.

For research use only. We do not sell to patients.

CGP 78608 hydrochloride Chemical Structure

CGP 78608 hydrochloride Chemical Structure

CAS No. : 1135278-54-4

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Based on 1 publication(s) in Google Scholar

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Description

CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 hydrochloride acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). Anticonvulsant activity[1][2].

IC50 & Target

NMDA Receptor

 

In Vitro

CGP-78608 hydrochloride decreases glycine sensitivity of GluN1/GluN3A receptors through an inter-subunit allosteric effect between GluN1 and GluN3A agonist-binding domain (ABD) sites[2].
CGP 78608 hydrochloride reduces or abolishes ammonia-dependent cGMP synthesis which is a causative factor of ammonia neurotoxicity[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CGP-78608 hydrochloride displays potent anticonvulsant effects after i.p. administration in the electroshock-induced convulsions assay in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

414.58

Formula

C11H14BrClN3O5P

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OP(O)([C@H](NCC1=CC(Br)=CC(NC2=O)=C1NC2=O)C)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

1 M NaOH : ≥ 50 mg/mL (120.60 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
1 M NaOH 1 mM 2.4121 mL 12.0604 mL 24.1208 mL 60.3020 mL
5 mM 0.4824 mL 2.4121 mL 4.8242 mL 12.0604 mL
10 mM 0.2412 mL 1.2060 mL 2.4121 mL 6.0302 mL
15 mM 0.1608 mL 0.8040 mL 1.6081 mL 4.0201 mL
20 mM 0.1206 mL 0.6030 mL 1.2060 mL 3.0151 mL
25 mM 0.0965 mL 0.4824 mL 0.9648 mL 2.4121 mL
30 mM 0.0804 mL 0.4020 mL 0.8040 mL 2.0101 mL
40 mM 0.0603 mL 0.3015 mL 0.6030 mL 1.5075 mL
50 mM 0.0482 mL 0.2412 mL 0.4824 mL 1.2060 mL
60 mM 0.0402 mL 0.2010 mL 0.4020 mL 1.0050 mL
80 mM 0.0302 mL 0.1508 mL 0.3015 mL 0.7538 mL
100 mM 0.0241 mL 0.1206 mL 0.2412 mL 0.6030 mL
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CGP 78608 hydrochloride Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CGP 78608 hydrochloride
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