1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. CGP52432

CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.

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

CGP52432 Chemical Structure

CGP52432 Chemical Structure

CAS No. : 139667-74-6

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 109 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

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  • Customer Review

Description

CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.

IC50 & Target

IC50: 85 nM (GABAB receptor)[1]

In Vitro

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.

In Vivo

CGP52432 (10, 30 mg/kg) shows no effect on the total arm entries and total head dips of mice on the elevated-plus maze[2]. CGP52432 (100 nmol/kg, i.v., or 1 nmol/kg, i.c.v.) abolishes the suppressive effects of GABA ( 50 μmol/kg, i.v.) on enhanced renal sympathetic nerve activity (RSNA) during ischaemia, causeing elimination of the renoprotective effects of GABA in rats[3].

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

Molecular Weight

384.24

Formula

C15H24Cl2NO4P

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=P(C(OCC)OCC)(CCCNCC1=CC=C(Cl)C(Cl)=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6025 mL 13.0127 mL 26.0254 mL
5 mM 0.5205 mL 2.6025 mL 5.2051 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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V1

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C2

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V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Animal Administration
[2]

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].

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

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, 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.

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Help & FAQs
  • 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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Product Name:
CGP52432
Cat. No.:
HY-103531
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