CGP 12177
CGP 12177 ((±)-CGP 12177) is a β-Adrenergic receptor (β-AR) ligand. CGP 12177 is a β3-AR (Ki = 88 nM) agonist with β1/β2-AR (Ki = 0.9 nM for β1; Ki = 4 nM for β2) antagonist action. CGP 12177 exhibits partial agonist properties for α1-AR in rat pulmonary artery. CGP 12177 regulates the expression of ucp and leptin genes in NMRI mice adipose tissues. CGP 12177 can be used for cardiovascular and metabolic disease research.
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- CAS No.: 81047-99-6
- Formule: C14H21N3O3
- Masse moléculaire:279.33
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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Beta-1 adrenergic receptor 0.9 nM (Ki) |
Beta-2 adrenergic receptor 4 nM (Ki) |
Beta-3 adrenergic receptor 88 nM (Ki) |
α1-adrenergic receptor |
CGP 12177 (0.01-100 μM) enhances tension induced by 3 μM Prostaglandin F2α (PGF2α) (HY-12956) in rat intralobar pulmonary arteries in a concentration-dependent manner, while inducing concentration-dependent relaxation when arteries precontracted with 30 nM Phenylephrine (PHE) (HY-B0769)[1].
CGP 12177 (0.01-100 μM) exerts only minor effect on rat intralobar pulmonary arteries under basal tone, but elicits contractile effects and markedly potentiates PHE-induced contraction in the presence of PGF2α (3 μM)[1].
CGP 12177 (1-100 μM) induces an increase in intracellular calcium concentration in rat pressurized arteries loaded with Fura pentakisester-3 (PE-3) and precontracted with PGF2α[1].
CGP 12177 (100 μM, 15 min) exhibits no significant effect on the basal tone in rat intralobar pulmonary arteries, but shifts the concentration-response curve to PHE to the right without any changes in the maximal response[1].
CGP 12177 (1–100 μM)-induced contractions in PGF2α-precontracted arteries are suppressed by Phentolamine (1 μM), Phenoxybenzamine (1 μM), SR 59230A (3 μM), and Bupranolol (5 μM) in rat intralobar pulmonary arteries[1].
CGP 12177 fully and concentration-dependently displaces [3H]prazosin-specific binding, with a pKi value of 5.22[1].
CGP 12177 (0-10 μM, 30 min) does not stimulate the internalization of GFP-tagged human β2-adrenoceptors in CHO-K1 cells[2].
CGP 12177 acts as a high-affinity partial agonist for cyclic AMP accumulation and cAMP response element (CRE)-mediated gene transcription in CHO-K1 cells expressing the human β2-adrenoceptor[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NMRI mice (4-weeks old)[3]
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Dosage:0.05, 0.2, 0.5 and 1mg/kg
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Administration:s.c., daily for 15 days
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Result:Significantly decreased expression of the mRNAs for UCP1, UCP2 and UCP3 in brown adipose tissue (BAT) at the lower doses compared to control.
Slightly increased expression of the mRNAs for UCP1, UCP2 and UCP3 in brown adipose tissue (BAT) at the higher doses compared to control.
Markedly enhanced UCP1 mRNA expression in both white adipose tissue (WAT) depots (inguinal IWAT and epididymal EWAT) in a dose-dependent manner, the increase was from low (and variable) basal levels in IWAT and from undetectable levels in EWAT of control animals.
Upregulated UCP3 mRNA expression in WAT especially in EWAT and, to a lesser extent, in IWAT.
Did not upregulated UCP2 mRNA expression in any WAT depot.
Showed a decreased expression of UCP2 mRNA at doses lower than 1mg/kg in both IWAT and EWAT.
Regulated leptin mRNA levels in a tissue-dependent manner.
Showed no effect on leptin mRNA levels in EWAT at any dose.
Showed a 3-fold increase of leptin mRNA levels in BAT at 0.5 and 1mg/kg.
Resulted in a maximum of 2-fold stimulation in IWAT at 0.5 mg/kg.
Did not have any apparent effect on food intake, body weight or the weight of the analysed fat depots at any dose tested.
Chemical Information
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CAS No. 81047-99-6
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Masse moléculaire 279.33
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Formule C14H21N3O3
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SMILES
O=C1NC2=C(OCC(O)CNC(C)(C)C)C=CC=C2N1
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Synonyms
(±)-CGP 12177
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Leblais V, et al. Role of alpha-adrenergic receptors in the effect of the beta-adrenergic receptor ligands, CGP 12177, bupranolol, and SR 59230A, on the contraction of rat intrapulmonary artery. J Pharmacol Exp Ther. 2004 Apr;309(1):137-45. [Content Brief]
[2]. Baker JG, et al. Pharmacological characterization of CGP 12177 at the human beta(2)-adrenoceptor. Br J Pharmacol. 2002 Oct;137(3):400-8. [Content Brief]
[3]. Oliver P, et al. In vivo effects of CGP-12177 on the expression of leptin and uncoupling protein genes in mouse brown and white adipose tissues. Int J Obes Relat Metab Disord. 2000 Apr;24(4):423-8. [Content Brief]
[4]. Strosberg AD, et al. Function and regulation of the beta 3-adrenoceptor. Trends Pharmacol Sci. 1996 Oct;17(10):373-81. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CGP 12177 Related Classifications
HY-101393 Related Classifications
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