Nebivolol 152520-56-4

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Molecular Weight: 441.9 Nebivolol selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.

Biological Activity

Nebivolol shows high affinity and selectivity for beta 1-adrenergic receptor sites in a rabbit lung membrane preparation (Ki value = 0.9 nM and beta 2/beta 1 ratio = 50). Nebivolol displays β1-adrenoceptor selectivity with the Ki(β2)/Ki(β1) value of 40.7 judged by competition experiments to 3H-CGP 12.1777 in the presence of CGP 207.12 A (300 nM, Kiβ2) or ICI 118.551 (50 nM, Kiβ1). Nebivolol reduces cell proliferation of human coronary smooth muscle
cells (haCSMCs) and endothelial cells (haECs) in a concentration- and
time-dependent maner.


Nebivolol treatment for 7 days causes significant
reduction in cell growth of haCSMCs with IC50 of 6.1 μM, and inhibits
accelerated haCSMC proliferation stimulated by growth factors PDGF-BB,
bFGF, and TGFβ with IC50 values of 6.8 μM, 6.4 μM and 7.7 μM,
repectively. Nebivolol treatment (10-5 M) of haCSMCs for 48
hours induces a moderate Apoptosis of 23% and a decrease from 16% to 5%
in the number of cells in S-phase. During Nebivolol incubation, NO
formation of HaCEs increases, while endothelin-1 transcription and
secretion are suppressed.


Administratiion of Nebivolol (initially by iv within 10 minutes of
reperfusion and then orally) to rats with myocardial infarction (MI)
reduces myocardial apoptosis, which is mediated by regulation of NO .
Nebivolol, significantly, prevents left ventricular (LV) pressure
changes, reduces total and regional apoptotic cardiomyocytes. Nebivolol
treatment lowers mean blood pressure (MBP) in rats with MI slightly,
but not significantly.



Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Download Nebivolol SDF

Molecular Weight (MW)	441.9
Formula	C22H25F2NO4.HCl
CAS No.	152520-56-4

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	88 mg/mL (199.14 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	2H-1-Benzopyran-2-methanol, α,α'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-, hydrochloride, [2R*[R*[R*(S*)]]]-(±)-

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Product Categories : Neuronal Signaling > Adrenergic Receptor Inhibitor