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Nebivolol

Cat. No. M3509
Nebivolol Structure
Size Price Availability Quantity
10mg USD 60 In stock
50mg USD 180 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Nebivolol (Bystolic) is a β1 receptor blocker with an IC50 of 4.5 µM. It has nitric oxide-potentiating vasodilatory effect used in treatment of hypertension. Nebivolol was compared with DETA-NO and S-nitroso-N-acetylpenicillamine (SNAP), two nitric oxide (NO) donor agents, and alpha-difluoromethylornithine (DFMO), a known inhibitor of ornithine decarboxylase (ODC). All four test agents inhibited RASMC proliferation in a concentration-dependent manner, with nebivolol being the most potent (IC (50) = 4.5 microM), whereas atenolol, another relatively selective beta (1)-blocker, was inactive.

Protocol
Cell Experiment
Cell lines Human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs)
Preparation method Exposing cells to different concentrations of Nebivolol (10-7~10-5 M) for 1, 2, 4, 7 and 14 days. Using bromodeoxyuridine (BrdU) incorporation to analyze cell proliferation , and PI or annexin V staining to detect cell apoptosis .
Concentrations Dissolved in 100% methanol and diluted with three volumes of growth medium to obtain a stock solution of 10-3 M, final concentration 10-7~10-5 M
Incubation time 1, 2, 4, 7 and 14 days
Animal Experiment
Animal models Male Sprague Dawley rat myocardial infarction (MI) model
Formulation Dissolved in DMSO and diluted in saline
Dosages 2.0 mg/kg
Administration Gastric gavage once daily
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 441.9
Formula C22H25F2NO4.HCl
CAS Number 152520-56-4
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Nebivolol supplier, Adrenergic Receptor, inhibitors

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