CGP55845 hydrochloride
Based on 2 publication(s) in Google Scholar
CGP55845 hydrochloride is a selective GABAB receptor competitive antagonist (IC50 = 5 nM). CGP55845 hydrochloride prevents agonist binding (pKi = 8.35). CGP55845 hydrochloride blocks presynaptic GABAB receptors, relieves the inhibition of GABA release, and blocks GABAB-mediated inhibitory signaling. CGP55845 hydrochloride restores long-term potentiation and novel object recognition memory in knockout mice.
For research use only. We do not sell to patients.
- Purity : 98.27%
- CAS No.: 149184-22-5
- Formula: C18H23Cl3NO3P
- Molecular Weight:438.71
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CGP55845 hydrochloride
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Biological Activity
Description
In Vitro
CGP55845 (1 µM) hydrochloride acts presynaptically to increase mIPSC frequency without altering quantal amplitude, mIPSC kinetics, or postsynaptic passive membrane properties in mouse Cajal-Retzius cells[1].
CGP55845 (1 µM) hydrochloride increases GABA release probability, reducing paired-pulse ratio and failure rate while attenuating paired-pulse correlation in mouse Cajal-Retzius cell GABAergic synapses[1].
CGP55845 (1 µM) hydrochloride reduces paired-pulse ratio across extracellular Ca2+ concentrations but does not change late eIPSC quantal amplitude in mouse Cajal-Retzius cells[1].
CGP 55845 (0.03-0.5 μM) hydrochloride is the most potent GABAB receptor antagonist tested in the hemisected rat spinal cord monosynaptic reflex assay, with an apparent Kd of 30.2 nM against (R)-Baclofen (HY-17354)-induced depression[3].
0.3 μM CGP55845 hydrochloride is as potent as 100 μM CGP35348 (HY-103530) in reversing the inhibitory effects of (R)-Baclofen[3].
CGP55845 (1 µM; 2-4 min) hydrochloride blocks IPSPB and increases NMDA EPSP duration and charge in dentate-hilus border interneurons, permitting a delayed polysynaptic burst[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CGP55845 (0.5 mg/kg; i.p.; single injection; 2 h before NOR familiarization) hydrochloride impaires NOR memory and reduces PSD95-positive puncta in the perirhinal cortex of healthy wild-type mice without altering spine density or maturation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 2 months old; Cdkl5 KO strain backcrossed to C57BL/6J for three generations)[2]
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Dosage:0.5 mg/kg
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Administration:i.p.; single injection; 2 h before NOR familiarization
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Result:Restored NOR memory in Cdkl5 -/Y mice.
Increased dendritic spine number, shifted the immature/mature spine balance toward mature spines, and increased PSD95-positive puncta in the perirhinal cortex of Cdkl5 -/Y mice.
Decreased spontaneous locomotor activity in Cdkl5 -/Y mice.
Chemical Information
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CAS No. 149184-22-5
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Appearance Solid
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Molecular Weight 438.71
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Formula C18H23Cl3NO3P
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Color White to off-white
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SMILES
O=P(CC1=CC=CC=C1)(C[C@@H](O)CN[C@H](C2=CC=C(Cl)C(Cl)=C2)C)O.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (227.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Kirmse K, et al. Ambient GABA constrains the strength of GABAergic synapses at Cajal-Retzius cells in the developing visual cortex. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2006 Apr 19;26(16):4216-27. [Content Brief]
[2]. Gennaccaro L, et al. A GABAB receptor antagonist rescues functional and structural impairments in the perirhinal cortex of a mouse model of CDKL5 deficiency disorder. Neurobiol Dis. 2021 Jun;153:105304. [Content Brief]
[3]. Brugger F, et al. The action of new potent GABAB receptor antagonists in the hemisected spinal cord preparation of the rat. Eur J Pharmacol. 1993 Apr 22;235(1):153-5. [Content Brief]
[4]. Salio C, et al. GABA receptors-mediated tonic inhibition of glutamate release from Aβ fibers in rat laminae III/IV of the spinal cord dorsal horn. Molecular pain. 2017;13:1744806917710041. [Content Brief]
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2794 mL | 11.3971 mL | 22.7941 mL | 56.9853 mL |
| 5 mM | 0.4559 mL | 2.2794 mL | 4.5588 mL | 11.3971 mL | |
| 10 mM | 0.2279 mL | 1.1397 mL | 2.2794 mL | 5.6985 mL | |
| 15 mM | 0.1520 mL | 0.7598 mL | 1.5196 mL | 3.7990 mL | |
| 20 mM | 0.1140 mL | 0.5699 mL | 1.1397 mL | 2.8493 mL | |
| 25 mM | 0.0912 mL | 0.4559 mL | 0.9118 mL | 2.2794 mL | |
| 30 mM | 0.0760 mL | 0.3799 mL | 0.7598 mL | 1.8995 mL | |
| 40 mM | 0.0570 mL | 0.2849 mL | 0.5699 mL | 1.4246 mL | |
| 50 mM | 0.0456 mL | 0.2279 mL | 0.4559 mL | 1.1397 mL | |
| 60 mM | 0.0380 mL | 0.1900 mL | 0.3799 mL | 0.9498 mL | |
| 80 mM | 0.0285 mL | 0.1425 mL | 0.2849 mL | 0.7123 mL | |
| 100 mM | 0.0228 mL | 0.1140 mL | 0.2279 mL | 0.5699 mL |
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