首页 GPCR/G Protein Histamine Receptor Bepotastine Besilate
Bepotastine Besilate
编号 T6405     别名: Bepotastine Beslilate, TAU 284, Bepreve, Talion, TAU 284, Talion, Bepreve, Bepotastine Beslilate
CAS 190786-44-8     分子式 C21H25ClN2O3·C6H6O3S     分子量 547.06
靶点: H1 receptor;
Bepotastine is a non-sedating and selective H1 receptor antagonist (pIC50: 5.7).
选择批次  
规格 库存 单价 数量
10 mg 上海现货 485.00
50 mg 上海现货 1745.00
100 mg 上海现货 2735.00
200 mg 上海现货 3282.00
500 mg 上海现货 7685.00
1 mL * 10 mM (in DMSO) 上海现货 530.00
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生物活性

产品描述

Bepotastine is a non-sedating and selective H1 receptor antagonist (pIC50: 5.7).

靶点活性

H1 receptor,5.7(pIC50)

体外活性

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. [2] Bepotastine besilate (100 mM) suppresses Leukotriene B(4) induced Ca(2+) concentration in cultured dorsal root ganglion neurons and cultured neutrophils. [3] 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. [4]

体内活性

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. [2] 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). [3] 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%. [4] 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. [5]

化学信息

分子量

547.06

分子式

C21H25ClN2O3·C6H6O3S

CAS

190786-44-8

溶解度

DMSO: 101 mg/mL (184.6 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 1.828 ml 9.14 ml 18.28 ml
5 mM 0.366 ml 1.828 ml 3.656 ml
10 mM 0.183 ml 0.914 ml 1.828 ml
50 mM 0.037 ml 0.183 ml 0.366 ml
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