CGP 12177
CAS No. : 81047-99-6
(Synonyms: (±)-CGP 12177)
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| Cat. No. : | HY-101393 |
| M.Wt: | 279.33 |
| Formula: | C14H21N3O3 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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[1][2][3][4].
In Vitro: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].
In Vivo:CGP 12177 (0.05, 0.2, 0.5 and 1mg/kg, s.c., daily for 15 days) stimulates the expression of certain ucp genes and the leptin gene concomitantly in NMRI mice adipose tissues[3].
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