| Identification | Back Directory | [Name]
CGP 20712 dihydrochloride | [CAS]
1216905-73-5 | [Synonyms]
1-[2-((3-Carbamoyl-4-hydroxy)phenoxy)ethylamino]-3-[4-(1-methyl-4-trifluoromethyl-2-imidazolyl)phenoxy]-2-propanol dihydrochloride | [Molecular Formula]
C23H26ClF3N4O5 | [MDL Number]
MFCD06798358 | [MOL File]
1216905-73-5.mol | [Molecular Weight]
530.93 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
≥16.25 mg/mL in H2O | [form ]
solid | [color ]
White to light yellow | [Water Solubility ]
Soluble to 50 mM in water |
| Hazard Information | Back Directory | [Uses]
CGP 20712 Dihydrochloride is a highly potent and selective β1-AR antagonist. | [Biological Activity]
cgp 20712 dihydrochloride is a potent and selective antagonist of β1-adrenoceptor with ic50 value of 0.7 nm [1].β1-adrenoceptor is a g-protein coupled receptor and mediates uncoupling protein-1 (ucp1) gene expression induced by norepinephrine (ne) [2].cgp 20712 dihydrochloride is a potent and selective β1-adrenoceptor antagonist. in neocortical membranes, cgp 20712 a exhibited affinity for β1-adrenoceptor and β2-adrenoceptor with ic50 values of 0.7 and 6700 nm, respectively [1]. in brown adipocytes, cgp-20712a significantly inhibited ucp1 gene expression induced by ne. however, cgp-20712a had no effect on lipolysis. these results suggested that β1-adrenoceptor mediated ucp1 gene expression [2]. in ventricular membranes from rats, cgp 20712a (300 nm) completely occupied its high-affinity binding sites. in ventricular myocytes isolated from rats, cgp 20712a (10, 100, 1000 nm) didn’t cause the activation of adenylate cyclase mediated by β2-adrenoceptors, which suggested that β2-adrenoceptors were not present on rat ventricular myocytes [3]. in adult rat cardiac myocytes, cgp 20712a inhibited β1-ar-stimulated apoptosis, which was mediated by a camp-dependent mechanism [4]. | [storage]
Desiccate at +4°C | [References]
[1]. dooley dj, bittiger h, reymann nc. cgp 20712 a: a useful tool for quantitating beta 1- and beta 2-adrenoceptors. eur j pharmacol, 1986, 130(1-2): 137-139.
[2]. chaudhry a, granneman jg. differential regulation of functional responses by beta-adrenergic receptor subtypes in brown adipocytes. am j physiol, 1999, 277(1 pt 2): r147-153.
[3]. kitagawa y, adachi-akahane s, nagao t. 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.
[4]. communal c, singh k, sawyer db, et al. opposing effects of beta(1)- and beta(2)-adrenergic receptors on cardiac myocyte apoptosis : role of a pertussis toxin-sensitive g protein. circulation, 1999, 100(22): 2210-2212. |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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