Bepotastine Besilate 190786-44-8

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight: 547.06 Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.

The flux ratios of [14C]Bepotastine (5 μM) in LLC-GA5-COL150 cells are
significantly greater than those in LLC-PK1, showing that the B-to-A
flux exceeds those in the other direction in LLC-GA5-COL150 cells.
Bepotastine stimulates P-gp-mediated ATP hydrolysis with Km, Vmax, and
Vmax/Km values of 1.25 mM, 108 nmol/min/mg protein, and 0.087 mL/min/mg
protein, respectively. Bepotastine besilate (100 mM)
suppresses Leukotriene B(4) induced Ca(2+) concentration in cultured
dorsal root ganglion neurons and cultured neutrophils. Bepotastine (100 μM) dose-dependently inhibits chemotaxis of cultured
guinea pig peritoneal eosinophils induced by LTB4. Bepotastine (1 mM)
significantly reduces A23187-induced histamine release of cultured rat
peritoneal mast cells.

Bepotastine (0.8 mg/kg) administrated in WT and P-gp KO mice results in
the plasma total concentrations 580 ng/mL and 467 ng/mL at 6 min after
dosing, respectively, and the plasma protein binding with 41.1% and
45.9%. The absorption of [14C]Bepotastine from the proximal region in
the presence and absence of verapamil is 63.0% and 72.4%, respectively,
and that from the distal region is 10.9% and 62.7%, respectively. Bepotastine besilate (10 mg/kg) inhibits scratching induced by an
intradermal injection of histamine (100 nmol/site), but not serotonin
(100 nmol/site). Bepotastine besilate (1 mg/kg-10 mg/kg, oral)
dose-dependently suppresses scratching induced by substance P (100
nmol/site) and leukotriene B(4) (0.03 nmol/site).


Bepotastine besilate significantly inhibits conjunctival vascular
hyperpermeability in a dose-dependent manner in guinea pig allergic
conjunctivitis models with maximal effect for Bepotastine besilate 1.5%. Bepotastine (3 mg/kg and 10 mg/kg) effectively inhibits
the compound 48/80-induced scratching behavior of BALB/c mice 1 hour
after oral administration. Bepotastine (10 mg/kg) also significantly
inhibits the scratching behavior and suppresses the serum LTB(4) levels
in atopic dermatitis model NC/Nga mice.





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)

Contact us if you need more details on 190786-44-8. We are ready to answer your questions on packaging, logistics, certification or any Other aspects about 190786-44-8 Bepotastine Besilate、Bepotastine Besilate 190786-44-8. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : Neuronal Signaling > Histamine Receptor Inhibitor