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Bepotastine Besilate(Bepreve)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bepotastine Besilate(Bepreve)图片
CAS NO:190786-44-8
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)547.06
FormulaC21H25ClN2O3.C6H6O3S
CAS No.190786-44-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 109 mg/mL (199.2 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Other info

Chemical Name: (S)-4-(4-((4-chlorophenyl)(pyridin-2-yl)methoxy)piperidin-1-yl)butanoic acid compound with benzenesulfonic acid (1:1)

InChi Key: UDGHXQPQKQPSBB-BOXHHOBZSA-N

InChi Code: InChI=1S/C21H25ClN2O3.C6H6O3S/c22-17-8-6-16(7-9-17)21(19-4-1-2-12-23-19)27-18-10-14-24(15-11-18)13-3-5-20(25)26;7-10(8,9)6-4-2-1-3-5-6/h1-2,4,6-9,12,18,21H,3,5,10-11,13-15H2,(H,25,26);1-5H,(H,7,8,9)/t21-;/m0./s1

SMILES Code: OC(CCCN1CCC(O[C@H](c2ncccc2)c3ccc(Cl)cc3)CC1)=O.OS(=O)(c4ccccc4)=O

SynonymsTAU 284; Bepotastine besylate; bepotastine besilate; TAU-284; TAU284; Bepreve; Talion.
实验参考方法
In Vitro

In vitro activity: 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.

In VivoBepotastine (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.
Animal modelMice
Formulation & Dosage1 mg/kg-10 mg/kg, oral
References

Drug Metab Dispos. 2006 May;34(5):793-9; Eur J Pharmacol. 2006 Oct 10;547(1-3):59-64.