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

Product information

CAS Number: 139667-74-6

Molecular Weight: 384.24

Formula: C15H24Cl2NO4P

Chemical Name: (3-{[(3,4-dichlorophenyl)methyl]amino}propyl)(diethoxymethyl)phosphinic acid

Smiles: CCOC(OCC)[P@](O)(=O)CCCNCC1C=C(Cl)C(Cl)=CC=1

InChiKey: GJZVQXWEIYRHBE-UHFFFAOYSA-N

InChi: InChI=1S/C15H24Cl2NO4P/c1-3-21-15(22-4-2)23(19,20)9-5-8-18-11-12-6-7-13(16)14(17)10-12/h6-7,10,15,18H,3-5,8-9,11H2,1-2H3,(H,19,20)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 5 mg/mL (13.01 mM; Need ultrasonic and warming). H2O : 4 mg/mL (10.41 mM; ultrasonic and warming and heat to 60°C).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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. 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.

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