(±)-Nebivolol-d4 (hydrochloride)
目录号 : GC46304
A neuropeptide with diverse biological activities
Cas No.:2701283-32-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(±)-Nebivolol-d4 is intended for use as an internal standard for the quantification of nebivolol by GC- or LC-MS. Nebivolol is a potent and selective β1-adrenergic receptor (β1-AR) antagonist (IC50s = 7.41 and 251 nM for β1- and β2-ARs, respectively, in a radioligand binding assay using rabbit lung membrane preparations).1 It is also selective for β1-ARs over serotonin 5-HT1A and 5-HT2, α1- and α2-adrenergic, histamine H1, and dopamine D2 receptors (IC50s = 27.5 and 2,239, 3,162 and >10,000, 5,623, and 10,000 nM, respectively). Nebivolol inhibits cAMP accumulation induced by norepinephrine in primary rat cardiac cells (IC50 = 22 nM) and induces vasodilation in mouse renal arteries via a nitric oxide- and cGMP-dependent mechanism (EC50 = 11.36 μM).2,3 It decreases contraction of isolated human left ventricular trabeculae induced by isoproterenol but does not exert intrinsic sympathomimetic activity (ISA).4 Nebivolol inhibits proliferation of human coronary artery smooth muscle cells (HCASMCs) in the presence and absence of growth factors (IC50s = 6.1, 6.8, 6.4, and 7.7 μM for HCASMCs grown in media containing no growth factor, PDGFBB, basic FGF, and TGF-β1, respectively).5 Formulations containing nebivolol have been used to treat hypertension.
1.Pauwels, P.J., Gommeren, W., Van Lommen, G., et al.The receptor binding profile of the new antihypertensive agent nebivolol and its stereoisomers compared with various beta-adrenergic blockersMol. Pharmacol.34(6)843-851(1988) 2.Pauwels, P.J., Leysen, J.E., and Janssen, P.A.β-adrenoceptor-mediated cAMP accumulation in cardiac cells: Effects of nebivololEur. J. Pharmacol.172(6)471-479(1989) 3.Georgescu, A., Pluteanu, F., Flonta, M.L., et al.Nebivolol induces a hyperpolarizing effect on smooth muscle cells in the mouse renal artery by activation of beta-2-adrenoceptorsPharmacology81(2)110-117(2008) 4.Brixius, K., Bundkirchen, A., BÖlck, B., et al.Nebivolol, bucindolol, metoprolol and carvedilol are devoid of intrinsic sympathomimetic activity in human myocardiumBr. J. Pharmacol.133(8)1330-1338(2001) 5.Brehm, B.R., Wolf, S.C., Bertsch, D., et al.Effects of nebivolol on proliferation and apoptosis of human coronary artery smooth muscle and endothelial cellsCardiovasc. Res.49(2)430-439(2001)
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2427 mL | 11.2133 mL | 22.4266 mL |
| 5 mM | 0.4485 mL | 2.2427 mL | 4.4853 mL |
| 10 mM | 0.2243 mL | 1.1213 mL | 2.2427 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。