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CGP-20712

Catalog No. T30846   CAS 137888-49-4
Synonyms: UNII-SIO2UEZ19H, CGP 20712

CGP-20712 is a selective β 1-adrenoceptor antagonist with an IC50 of 0.7 nM.

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CGP-20712 Chemical Structure
CGP-20712, CAS 137888-49-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 350.00
5 mg In stock $ 828.00
10 mg In stock $ 1,130.00
25 mg In stock $ 1,590.00
50 mg In stock $ 1,980.00
100 mg In stock $ 2,500.00
500 mg In stock $ 4,900.00
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Purity: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CGP-20712 is a selective β 1-adrenoceptor antagonist with an IC50 of 0.7 nM.
Targets&IC50 β1-adrenoceptor:0.7 nM, β2-adrenoceptor:6700 nM
In vitro In brown adipocytes, CGP-20712 (1 μM) significantly inhibited UCP1 gene expression induced by NE. However, CGP-20712 had no effect on lipolysis. These results suggested that β1-adrenoceptor mediated UCP1 gene expression.[4]
In neocortical membranes, CGP 20712 exhibited affinity for β1-adrenoceptor and β2-adrenoceptor with IC50 values of 0.7 and 6700 nM, respectively.[1]
In vivo CGP 20712 (a selective beta 1-adrenergic receptor antagonist) (5 mg/kg; Pretreatment of 8-day-old rats) did not change the plasma ACTH response to insulin injection.[3]
Synonyms UNII-SIO2UEZ19H, CGP 20712
Molecular Weight 494.46
Formula C23H25F3N4O5
CAS No. 137888-49-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Dooley DJ, et al. Quantitative assessment of central beta 1- and beta 2-adrenoceptor regulation using CGP 20712 A. J Pharmacol Methods. 1987 Sep;18(2):131-6. 2. Kitagawa Y, et al. Determination of beta-adrenoceptor subtype on rat isolated ventricular myocytes by use of highly selective beta-antagonists. Br J Pharmacol. 1995;116(1):1635-1643. 3. Grino M, et al. Ontogeny of insulin-induced hypoglycemia stimulation of adrenocorticotropin secretion in the rat: role of catecholamines. Endocrinology. 1992;131(6):2763-2768. 4. Chaudhry A, et al. Differential regulation of functional responses by beta-adrenergic receptor subtypes in brown adipocytes. Am J Physiol. 1999;277(1):R147-R153.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library

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Keywords

CGP-20712 137888-49-4 GPCR/G Protein Neuroscience Adrenergic Receptor UNII-SIO2UEZ19H CGP 20712 CGP20712 inhibitor inhibit

 

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