Shanghai Nianxing Industrial Co., Ltd
China
Product Name: CGP 52432
Price:
Purity: 99.0%
Stocking Period: 10 Day
Contact: Yang

ShangHai DC Chemicals Co.,Ltd
China
Product Name: CGP 52432
Price: ￥Inquiry/1g
Purity: 98.9%
Stocking Period: 1 Day
Contact: Tony Lai

DC Chemicals Limited
China
Product Name: CGP 52432
Price: $600.0/100mg $1100.0/250mg $2100.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

139667-74-6

139667-74-6 structure

139667-74-6 structure

Name: CGP 52432
Chemical Name: 3-[(3,4-dichlorophenyl)methylamino]propyl-(diethoxymethyl)phosphinic acid
CAS Number: 139667-74-6
Molecular Formula: C₁₅H₂₄Cl₂NO₄P
Molecular Weight: 384.23500
Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
Create Date: 2018-08-27 12:48:51
Modify Date: 2024-01-27 21:40:21
CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.

Name	3-[(3,4-dichlorophenyl)methylamino]propyl-(diethoxymethyl)phosphinic acid
Synonyms	Tocris-1246 MFCD00041095 [3-[[(3,4-Dichlorophenyl)methyl]amino]propyl](diethoxymethyl)-phosphinic acid CGP52432

Description	CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor Signaling Pathways >> Neuronal Signaling >> GABA Receptor Research Areas >> Neurological Disease
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].
Animal Admin	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].
References	[1]. Lanza M, et al. 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. [2]. Sweeney FF, et al. Activation but not blockade of GABAB receptors during early-life alters anxiety in adulthood in BALB/c mice. Neuropharmacology. 2014 Jun;81:303-10. [3]. Kobuchi S, et al. 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.

Density	1.258g/cm3
Boiling Point	544.4ºC at 760mmHg
Molecular Formula	C₁₅H₂₄Cl₂NO₄P
Molecular Weight	384.23500
Flash Point	283.1ºC
Exact Mass	383.08200
PSA	77.60000
LogP	4.49100
Vapour Pressure	1.1E-12mmHg at 25°C
Index of Refraction	1.524
Storage condition	2-8℃

RIDADR	NONH for all modes of transport