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MedKoo Cat#: 524641 | Name: CGP52432
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

CGP52432 is a GABA-A receptor antagonist

Chemical Structure

CGP52432
CGP52432
CAS#139667-74-6

Theoretical Analysis

MedKoo Cat#: 524641

Name: CGP52432

CAS#: 139667-74-6

Chemical Formula: C15H24Cl2NO4P

Exact Mass: 383.0820

Molecular Weight: 384.24

Elemental Analysis: C, 46.89; H, 6.30; Cl, 18.45; N, 3.65; O, 16.66; P, 8.06

Price and Availability

Size Price Availability Quantity
50mg USD 550.00 2 Weeks
100mg USD 950.00 2 Weeks
200mg USD 1,450.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 3,750.00 2 Weeks
2g USD 6,250.00 2 Weeks
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Related CAS #
No Data
Synonym
CGP52432; CGP-52432; CGP 52432;
IUPAC/Chemical Name
Phosphinic acid, (3-(((3,4-dichlorophenyl)methyl)amino)propyl)(diethoxymethyl)-
InChi Key
GJZVQXWEIYRHBE-UHFFFAOYSA-N
InChi Code
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)
SMILES Code
O=P(C(OCC)OCC)(CCCNCC1=CC=C(Cl)C(Cl)=C1)O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
In vitro activity:
The novel GABAB receptor antagonist, [3-[[(3,4-dichlorophenyl)methyl]amino]propyl](diethoxy-methyl) phosphinic acid (CGP 52432), was investigated on the above receptor subtypes. The effects of (-)-baclofen on the K(+)-evoked release of GABA, glutamate or somatostatin from rat cortical synaptosomes were antagonized by CGP 52432. The IC50 of the drug at GABA autoreceptors (0.085 microM) was 35- and 100-fold lower than at the receptors regulating somatostatin and glutamate overflow, respectively. At the autoreceptor the calculated pA2 for CGP 52432 amounted to 7.70, which makes the drug about 1000-fold more potent than phaclofen at this receptor. The potency and selectivity characteristics of CGP 52432 indicate that the drug is by far the most appropriate tool to investigate the terminal GABAB autoreceptors of the rat cerebral cortex. Reference: Eur J Pharmacol. 1993 Jun 24;237(2-3):191-5. https://linkinghub.elsevier.com/retrieve/pii/0014-2999(93)90268-M
In vivo activity:
Male BALB/c mouse pups were treated with the either the selective GABAB receptor agonist, R-baclofen (2 mg/kg, s.c), the GABAB receptor antagonist CGP 52432 (10 mg/kg and 30 mg/kg) or vehicle from postnatal days (P) 14-28. The anxiety behaviour of these mice was then assessed in adulthood (P62 onwards) in a battery of behavioural tests comprising; the stress induced hyperthermia (SIH) test, defensive marble burying (DMB), elevated-plus maze (EPM) and the forced swim test (FST). Postnatal R-baclofen treatment resulted in increased anxiety-like behaviour in the EPM as shown by approach-avoidance and ethological measures. Other behavioural measures were not significantly altered. Interestingly, blockade of GABAB receptors with CGP52432 in early life caused no alterations in emotional behaviour. These data suggest that during early life GABAB receptor signalling can play a functional role in programing anxiety behaviour in adulthood. The underlying neurodevelopmental processes underlying these effects remain to be discovered. Reference: Neuropharmacology. 2014 Jun;81:303-10. https://linkinghub.elsevier.com/retrieve/pii/S0028-3908(13)00407-3
Solvent mg/mL mM
Solubility
DMSO 5.0 13.01
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 384.24 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
1. Lanza M, Fassio A, Gemignani A, Bonanno G, Raiteri M. 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. doi: 10.1016/0014-2999(93)90268-m. PMID: 8103461.
In vivo protocol:
1. Sweeney FF, O'Leary OF, Cryan JF. Activation but not blockade of GABAB receptors during early-life alters anxiety in adulthood in BALB/c mice. Neuropharmacology. 2014 Jun;81:303-10. doi: 10.1016/j.neuropharm.2013.08.039. Epub 2013 Sep 17. PMID: 24050962. 2. Kobuchi S, Tanaka R, Shintani T, Suzuki R, Tsutsui H, Ohkita M, Matsumura Y, Ayajiki K. 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. doi: 10.1111/1440-1681.12350. PMID: 25482107.
1: Jackson GL, Kuehl D. The GABA(B) antagonist CGP 52432 attenuates the stimulatory effect of the GABA(B) agonist SKF 97541 on luteinizing hormone secretion in the male sheep. Exp Biol Med (Maywood). 2002 May;227(5):315-20. PubMed PMID: 11976401. 2: Lanza M, Fassio A, Gemignani A, Bonanno G, Raiteri M. 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. PubMed PMID: 8103461.