KUL-7211
KUL 7211 is a selective β-adrenoceptor agonist.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 220129-58-8
- 分子式: C19H23NO5
- 分子量:345.39
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Adrenergic Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
β-adrenoceptor[1]
KUL 7211 (KUL-7211) is a new β-adrenoceptor agonist in vitro. In rat isolated organs, its selectivities, for inhibition of spontaneous uterine contraction (mediated via β2-adrenergic stimulation) and inhibition of colonic contraction (via β3-adrenergic stimulation) versus increase in atrial rate (via β1-adrenergic stimulation), are 56.3 and 242.2, respectively. KUL 7211 relaxes 80 mM KCl induced tonic contractions in both rabbit (pD2 value: 5.86±0.13, whose ureteral relaxation is mediated via β2-adrenergic stimulation) and canine (pD2 value: 6.52±0.16, via β3-adrenergic stimulation) isolated ureters in a concentration-dependent manner. These KUL 7211-induced relaxing effects are antagonized by ICI-118,551 (selective β2-adrenoceptor antagonist, pKB value: 8.91±0.24) in the rabbit ureter and by bupranolol (non-selective β-adernoceptor antagonist, pKB value: 6.85±0.12) in the canine ureter. KUL 7211 also reduces the spontaneous rhythmic contraction in a canine ureteral spiral preparation in a concentration-dependent manner, the pD2 value being 6.83±0.20. These data clearly demonstrate that KUL 7211 selectively stimulates both ureteral β2- and β3-adrenoceptors and potently relaxes ureteral smooth muscle[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
CAS 番号 220129-58-8
-
分子量 345.39
-
分子式 C19H23NO5
-
SMILES
O=C(O)COC1=CC=C(CCN[C@@H](C)[C@H](O)C2=CC=C(O)C=C2)C=C1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
KUL 7211 (KUL-7211) is dissolved in distilled water with an equivalent molarity of HCl[1].
Experiments are carried out using rat isolated atria, uterus, and proximal colon. Rats are stunned and then killed by rapid exsanguination. Each organ is rapidly removed and suspended in a 10 or 20 mL organ bath. The bath solution is Krebs solution (118.1 mM NaCl, 4.7 mM KCl, 2.5 mM CaCl2, 1.2 mM MgSO4• 7H2O, 25.0 mM NaHCO3, 1.2 mM KH2PO4, 11.1 mM glucose) in the atria and colon experiments and Locke-Ringer solution (154 mM NaCl, 5.6 mM KCl, 2.6 mM CaCl2, 2.1 mM MgCl2, 6.0 mM NaHCO3, 2.8 mM glucose) in the uterus experiment. Each is continuously gassed with a mixture of 95% oxygen and 5% carbon dioxide at 37°C. The bath solutions contain 1 μM phentolamine, 0.5μM desipramine, and 3 0μ M hydrocortisone to block α-adrenoceptors and neuronal and extraneuronal catecholamine uptake, respectively. Spontaneous contractions are measured isometrically by means of a force-transducer and measuring system (TB-611T, AP-601G, and RPM-6004 or model 45196A, model 1829, and model 7903) connected to a thermowriting rectigraph. An initial resting tension of 5 mN is placed on each organ, and it is allowed to equilibrate for 1 h. Each preparation is exposed to only one drug[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)