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

CGP52432 

Cat. No.: HY-103531 Purity: 98.50%
Handling Instructions

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 USD 99 In-stock
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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].

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].

Molecular Weight

384.24

Formula

C₁₅H₂₄Cl₂NO₄P

CAS No.

139667-74-6

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (13.01 mM; Need ultrasonic and warming)

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
10 mM 0.2603 mL 1.3013 mL 2.6025 mL
*Please refer to the solubility information to select the appropriate solvent.
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
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CGP52432
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