(±)-Nebivolol-d4 (hydrochloride) |
| カタログ番号GC46304 |
多様な生物学的活性を持つ神経ペプチド
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2701283-32-9
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
(±)-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)
| Cas No. | 2701283-32-9 | SDF | |
| Canonical SMILES | FC1=CC=C2C(CCC(C(O)C([2H])([2H])NC([2H])([2H])C(O)C3CCC(C=C(F)C=C4)=C4O3)O2)=C1.Cl | ||
| Formula | C22H21D4F2NO4.HCl | M.Wt | 445.9 |
| 溶解度 | DMSO: soluble | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *