CGP52432
featured

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

MedKoo CAT#: 524641

CAS#: 139667-74-6

Description: CGP52432 is a GABA-A receptor antagonist

Chemical Structure

img
CGP52432
CAS# 139667-74-6
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 524641
Name: CGP52432
CAS#: 139667-74-6
Chemical Formula: C15H24Cl2NO4P
Exact Mass: 383.08
Molecular Weight: 384.240
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 2 Weeks
100mg USD 950 2 Weeks
200mg USD 1450 2 Weeks
500mg USD 2650 2 Weeks
1g USD 3750 2 Weeks
2g USD 6250 2 Weeks
Bulk inquiry

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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 5.0 13.01

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.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

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.