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この商品について
実験式(ヒル表記法):
C14H21N3O3 · HCl
CAS番号:
分子量:
315.80
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
製品名
(±)-CGP-12177A, ≥98% (HPLC), solid
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
SMILES string
Cl.CC(C)(C)NCC(O)COc1cccc2NC(=O)Nc12
InChI key
YQVFCYCTITZLSX-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
color
white
solubility
DMSO: >10 mg/mL
Quality Level
Gene Information
human ... ADRB1(153), ADRB2(154), ADRB3(155)
Biochem/physiol Actions
β-アドレナリンレセプタ-の非従来型の部分アゴニストです。
Application
(±)-CGP-12177A has been used as a β-Adrenergic receptor agonist:
- to evaluate the dissociation constant (Kd) by frontal affinity chromatography
- to study its cardiostimulant effects on rat ventricular cardiomyocytes
- to study its binding affinity in α1D-adrenoceptors expressed in rat BHK-21 cells
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
J Oostendorp et al.
British journal of pharmacology, 130(4), 747-758 (2000-06-24)
The smooth muscle relaxant responses to the mixed beta(3)-, putative beta(4)-adrenoceptor agonist, (-)-CGP 12177 in rat colon are partially resistant to blockade by the beta(3)-adrenoceptor antagonist SR59230A suggesting involvement of beta(3)- and putative beta(4)-adrenoceptors. We now investigated the function of
P Oliver et al.
International journal of obesity and related metabolic disorders : journal of the International Association for the Study of Obesity, 24(4), 423-428 (2000-05-11)
To assess the effect of chronic treatment with CGP-12177 a beta3-adrenergic receptor (AR) agonist with beta2/beta1-AR antagonist action, on the expression of the leptin gene and of genes coding for uncoupling proteins (ucp1, ucp2 and ucp3) in brown and white
Maura Floreani et al.
European journal of pharmacology, 590(1-3), 303-309 (2008-07-01)
Recent in vitro studies, performed in rat aorta, mesenteric and intrapulmonary arteries, and human pulmonary artery, demonstrated that the beta-adrenoceptor ligand CGP-12177A (4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2H-benzimidazol-2-one) is also provided with antagonist or partial agonist properties at alpha(1)-adrenoceptors. These observations were supported by estimates
Clive J Lewis et al.
British journal of pharmacology, 141(5), 813-824 (2004-02-06)
1. CGP 12177A mediates cardiostimulation by activation of the 'putative' beta(4)-adrenoceptor; however, it has recently been reported that disruption of the beta(1)-adrenoceptor gene abolishes this effect. We have adenovirally overexpressed beta(1)-adrenoceptors in isolated, cultured adult rat ventricular cardiomyocytes and observed
Y Yamamoto et al.
Journal of smooth muscle research = Nihon Heikatsukin Gakkai kikanshi, 36(1), 13-19 (2000-06-01)
In the present study, we tried to determine what effects were induced by beta-adrenoceptor agonists on 40 mM KCl-induced rhythmic contraction and to clarify which beta-adrenoceptor subtypes are involved in the regulation of ureter motility in the guinea pig by
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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