CGP52432
Based on 8 publication(s) in Google Scholar
CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
For research use only. We do not sell to patients.
- Purity: 98.57%
- CAS No.: 139667-74-6
- Formula: C15H24Cl2NO4P
- Molecular Weight:384.24
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CGP52432
More- Signal Transduct Target Ther. 2026 Apr 24;11(1):150. [Abstract]
- Nat Neurosci. 2025 Jul;28(7):1404-1417. [Abstract]
- Adv Sci (Weinh). 2025 Oct 20:e07908. [Abstract]
- Stem Cell Res Ther. 2021 Jan 7;12(1):22. [Abstract]
- Brain Res Bull. 2025 Feb:221:111217. [Abstract]
- Am J Physiol Endocrinol Metab. 2025 Mar 24. [Abstract]
- Fish Shellfish Immunol. 2023 Mar:134:108608. [Abstract]
- Rev Port Cardiol. 2023 Feb;42(2):125-135. [Abstract]
Biological Activity
IC50: 85 nM (GABAB receptor)[1]
CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM, 35- and 100-fold lower than at the receptors regulating somatostatin and glutamate overflow, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 139667-74-6
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Appearance Solid
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Molecular Weight 384.24
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Formula C15H24Cl2NO4P
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Color White to off-white
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SMILES
O=P(C(OCC)OCC)(CCCNCC1=CC=C(Cl)C(Cl)=C1)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Endothelial GABA protects against aortic dissection by inhibiting endothelial and mitochondrial dysfunction and maintaining vascular homeostasis. [Abstract]2026 Apr 24;11(1):150. PMID: 42031717 -
Nat Neurosci
GABA-dependent microglial elimination of inhibitory synapses underlies neuronal hyperexcitability in epilepsy. [Abstract]2025 Jul;28(7):1404-1417. PMID: 40425792 -
Adv Sci (Weinh)
Morphine Tolerance Gated through EZH2-Mediated Suppression of Trpc5 in Spinal GABAergic Interneurons in Male Mice. [Abstract]2025 Oct 20:e07908. PMID: 41111460 -
Stem Cell Res Ther
GABAB receptor antagonist promotes hippocampal neurogenesis and facilitates cognitive function recovery following acute cerebral ischemia in mice. [Abstract]2021 Jan 7;12(1):22. PMID: 33413637 -
Brain Res Bull
GABAB receptors regulate the neural stem cell potential of Pkd2l1+ cerebrospinal fluid-contacting neurons via the PI3K/Akt signaling pathway. [Abstract]2025 Feb:221:111217. PMID: 39842645 -
Am J Physiol Endocrinol Metab
GLP-1 receptor agonist exendin-4 suppresses food intake by inhibiting hindbrain orexigenic NPY neurons. [Abstract]2025 Mar 24. PMID: 40126941 -
Fish Shellfish Immunol
Gamma-aminobutyric acid (GABA) suppresses hemocyte phagocytosis by binding to GABA receptors and modulating corresponding downstream pathways in blood clam, Tegillarca granosa. [Abstract]2023 Mar:134:108608. PMID: 36764632 -
Rev Port Cardiol
The protective effect of gamma aminobutyric acid B receptor activation on sympathetic nerve remodeling via the regulation of M2 macrophage polarization after myocardial infarction. [Abstract]2023 Feb;42(2):125-135. PMID: 36759072
Solvent & Solubility
DMSO : 5 mg/mL (13.01 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 4 mg/mL (10.41 mM; ultrasonic and warming and heat to 60°C)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Mice[2]
Two separate cohorts of male pups are used for the study. One cohort is treated with either R(+)baclofen HCl (2 mg/kg) or with vehicle (PBS). The second cohort is treated with the GABAB receptor antagonist CGP52342 (10, 30 mg/kg) or vehicle (PBS). Drugs are freshly prepared for injection each day, by dissolution in PBS with vortexing and brief sonication. Doses of R(+)baclofen and CGP52432 are chosen to be well tolerated in adult mice. All drug treatments are given via subcutaneous injection, once daily from P14-28 in a volume of 0.05 mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lanza M, et al. CGP 52432: a novel potent and selective GABAB autoreceptor antagonist in rat cerebral cortex. Eur J Pharmacol. 1993 Jun 24;237(2-3):191-5. [Content Brief]
[2]. Sweeney FF, et al. Activation but not blockade of GABAB receptors during early-life alters anxiety in adulthood in BALB/c mice. Neuropharmacology. 2014 Jun;81:303-10. [Content Brief]
[3]. Kobuchi S, et al. Mechanisms underlying the renoprotective effect of GABA against ischaemia/reperfusion-induced renal injury in rats. Clin Exp Pharmacol Physiol. 2015 Mar;42(3):278-86. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.6025 mL | 13.0127 mL | 26.0254 mL | 65.0635 mL |
| 5 mM | 0.5205 mL | 2.6025 mL | 5.2051 mL | 13.0127 mL | |
| 10 mM | 0.2603 mL | 1.3013 mL | 2.6025 mL | 6.5064 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
CGP52432 Related Classifications
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