CGP 12177 (hydrochloride)
CAS No. : 64208-32-8
(Synonyms: (±)-CGP 12177 (hydrochloride))
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| Cat. No. : | HY-101393A |
| M.Wt: | 315.80 |
| Formula: | C14H22ClN3O3 |
| Purity: | >98 % |
| Solubility: | DMSO : 10 mg/mL (ultrasonic) |
CGP 12177 ((±)-CGP 12177) hydrochloride is a β-Adrenergic receptor (β-AR) ligand. CGP 12177 hydrochloride 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 hydrochloride exhibits partial agonist properties for α1-AR in rat pulmonary artery. CGP 12177 hydrochloride regulates the expression of ucp and leptin genes in NMRI mice adipose tissues. CGP 12177 hydrochloride can be used for cardiovascular and metabolic disease research[1][2][3][4].
In Vitro:CGP 12177 (0.01-100 μM) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride-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 hydrochloride fully and concentration-dependently displaces [3H]prazosin-specific binding, with a pKi value of 5.22[1].
CGP 12177 (0-10 μM, 30 min) hydrochloride does not stimulate the internalization of GFP-tagged human β2-adrenoceptors in CHO-K1 cells[2].
CGP 12177 hydrochloride 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) hydrochloride stimulates the expression of certain ucp genes and the leptin gene concomitantly in NMRI mice adipose tissues[3].
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