CGP 12177 hydrochlorideβ1/β2-AR antagonist,β3 AR partial agonist CAS# 64208-32-8 |
Quality Control & MSDS
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| Cas No. | 64208-32-8 | SDF | Download SDF |
| PubChem ID | 11957517 | Appearance | Powder |
| Formula | C14H22ClN3O3 | M.Wt | 315.8 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in water | ||
| Chemical Name | 4-[3-(tert-butylamino)-2-hydroxypropoxy]-1,3-dihydrobenzimidazol-2-one;hydrochloride | ||
| SMILES | CC(C)(C)NCC(COC1=CC=CC2=C1NC(=O)N2)O.Cl | ||
| Standard InChIKey | YQVFCYCTITZLSX-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C14H21N3O3.ClH/c1-14(2,3)15-7-9(18)8-20-11-6-4-5-10-12(11)17-13(19)16-10;/h4-6,9,15,18H,7-8H2,1-3H3,(H2,16,17,19);1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Partial agonist at β3-adrenoceptors. β1- and β2-adrenoceptor antagonist (Ki values are 0.9, 4 and 88 nM for β1, β2 and β3 receptors respectively). |
CGP 12177 hydrochloride Dilution Calculator
CGP 12177 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.1666 mL | 15.8328 mL | 31.6656 mL | 63.3312 mL | 79.164 mL |
| 5 mM | 0.6333 mL | 3.1666 mL | 6.3331 mL | 12.6662 mL | 15.8328 mL |
| 10 mM | 0.3167 mL | 1.5833 mL | 3.1666 mL | 6.3331 mL | 7.9164 mL |
| 50 mM | 0.0633 mL | 0.3167 mL | 0.6333 mL | 1.2666 mL | 1.5833 mL |
| 100 mM | 0.0317 mL | 0.1583 mL | 0.3167 mL | 0.6333 mL | 0.7916 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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CGP 12177 hydrochloride is a partial agonist of β3-adrenoceptor and an antagonist of β1- and β2-adrenoceptors with Ki values of 0.9, 4 and 88 nM for β1-, β2- and β3-adrenoceptors, respectively.
β3-adrenoceptor is exists mainly in adipose tissue and plays an important role in the regulation of thermogenesis and lipolysis.
CGP 12177 hydrochloride is a partial agonist of β3-adrenoceptor and an antagonist of β1- and β2-adrenoceptors. In human ventricular myocytes (HVMs), CGP12177 slightly activated L-type Ca2+ current (ICa,L) [1].
In sympathectomized (SX) interscapular brown adipose tissue (BAT) isolated from rats, CGP-12177 restored normal thyroxine (T4) deiodination, which suggested that CGP-12177 activated 5’-deiodinase type II through β3-adrenoceptor [2]. In spontaneously hypertensive rats (SHR) and normotensive rats, CGP12177 induced vasorelaxant effects and decreased hindquarters
perfusion pressure in a dose-dependent way induced by 5-hydroxytryptamine (5-HT), which was inhibited by bupranolol, a β1LA-adrenoceptor antagonist. These results suggested that CGP12177 induced vasorelaxant effects through activation of β1LA-adrenoceptor [3].
References:
[1]. Treinys R, Zablockaitė D, Gendvilienė V, et al. β₃-Adrenergic regulation of L-type Ca²⁺ current and force of contraction in human ventricle. J Membr Biol, 2014, 247(4): 309-318.
[2]. Hofer D, Raíces M, Schauenstein K, et al. The in vivo effects of beta-3-receptor agonist CGP-12177 on thyroxine deiodination in cold-exposed, sympathectomized rat brown fat. Eur J Endocrinol, 2000, 143(2): 273-277.
[3]. Holopherne D, Mallem MY, Le Strat E, et al. CGP12177-induced haemodynamic and vascular effects in normotensive and hypertensive rats. Eur J Pharmacol, 2008, 591(1-3): 196-202.
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Metabolic response to various beta-adrenoceptor agonists in beta3-adrenoceptor knockout mice: evidence for a new beta-adrenergic receptor in brown adipose tissue.[Pubmed:9756384]
Br J Pharmacol. 1998 Aug;124(8):1684-8.
The beta3-adrenoceptor plays an important role in the adrenergic response of brown and white adipose tissues (BAT and WAT). In this study, in vitro metabolic responses to beta-adrenoceptor stimulation were compared in adipose tissues of beta3-adrenoceptor knockout and wild type mice. The measured parameters were BAT fragment oxygen uptake (MO2) and isolated white adipocyte lipolysis. In BAT of wild type mice (-)-norepinephrine maximally stimulated MO2 4.1+/-0.8 fold. Similar maximal stimulations were obtained with beta1-, beta2- or beta3-adrenoceptor selective agonists (dobutamine 5.1+/-0.3, terbutaline 5.3+/-0.3 and CL 316,243 4.8+/-0.9 fold, respectively); in BAT of beta3-adrenoceptor knockout mice, the beta1- and beta2-responses were fully conserved. In BAT of wild type mice, the beta1/beta2-antagonist and beta3-partial agonist CGP 12177 elicited a maximal MO2 response (4.7+/-0.4 fold). In beta3-adrenoceptor knockout BAT, this response was fully conserved despite an absence of response to CL 316,243. This unexpected result suggests that an atypical beta-adrenoceptor, distinct from the beta1-, beta2- and beta3-subtypes and referred to as a putative beta4-adrenoceptor is present in BAT and that it can mediate in vitro a maximal MO2 stimulation. In isolated white adipocytes of wild type mice, (-)-epinephrine maximally stimulated lipolysis 12.1+/-2.6 fold. Similar maximal stimulations were obtained with beta1-, beta2- or beta3-adrenoceptor selective agonists (TO509 12+/-2, procaterol 11+/-3, CL 316,243 11+/-3 fold, respectively) or with CGP 12177 (7.1+/-1.5 fold). In isolated white adipocytes of beta3-adrenoceptor knockout mice, the lipolytic responses to (-)epinephrine, to the beta1-, beta2-, beta3-adrenoceptor selective agonists and to CGP 12177 were almost or totally depressed, whereas those to ACTH, forskolin and dibutyryl cyclic AMP were conserved.
Function and regulation of the beta 3-adrenoceptor.[Pubmed:8979772]
Trends Pharmacol Sci. 1996 Oct;17(10):373-81.
The cloning, sequencing and expression in model systems of the previously unidentified beta 3-adrenoceptor recently led to an extensive functional characterization. Ligand binding and adenylate cyclase activation studies helped define a specific profile that is quite distinct from that of the beta 1- and beta 2-adrenoceptors, but strongly reminiscent of most of the 'atypical' beta-adrenoceptor-mediated responses reported in earlier pharmacological studies. More recently, a naturally occurring variation in the human beta 3-adrenoceptor has been correlated with hereditary obesity and with increased dynamic capacity to add on weight and develop non-insulin dependent diabetes in Western obese patients. Donny Strosberg and France Pietri-Rouxel describe how results now provide a consistent picture of an important role for the human beta 3-adrenoceptor in the regulation of lipid metabolism and as an obvious target for drugs to treat some forms of obesity and diabetes.
CGP-12177. A hydrophilic beta-adrenergic receptor radioligand reveals high affinity binding of agonists to intact cells.[Pubmed:6131886]
J Biol Chem. 1983 Mar 25;258(6):3496-502.
A new, hydrophilic beta-adrenergic receptor radioligand, (+/-)-[3H]CGP-12177 (4-(3-tertiarybutylamino-2-hydroxypropoxy)-benzimidazole-2-on hydrochloride), was synthesized and radiolabeled to 40 Ci/mmol. The nonspecific binding of this compound to turkey erythrocyte ghosts and C6 glioma cell membranes was less than 5% of the total binding at five times the appropriate KD. Binding assays of intact C6 glioma cells also showed low nonspecific binding, less than 20% of the total binding at five times the appropriate KD. The affinities of the antagonists (-)- and (+)-propranolol as well as of the agonist (-)-isoproterenol were examined by their potency to displace various radioligands from intact C6 glioma cell and membrane preparations. With membrane preparations, both [3H] CGP-12177 and [3H]dihydroalprenolol (DHA) were displaced stereospecifically by the antagonists (-)- and (+)-propranolol and the agonist (-)-isoproterenol. With whole cells, [3H]CGP-12177 and [3H]DHA behaved differently. [3H]DHA and [3H]carazolol could be stereospecifically displaced by antagonists but only partially displaced by agonists, while [3H]CGP-12177 could be completely displaced by both antagonists and agonists as in membranes. In contrast to [3H]CGP-12177, the lipophilic ligand [3H]DHA is actually taken up by cells. The inability of agonists to displace lipophilic radioligands from receptors on intact cells may not be due to a low affinity of agonists for receptors on cells, but to an agonist-induced change in the receptors which renders them inaccessible to hydrophilic agonists and antagonists. This change is likely to be their internalization into the cell.
