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Bepotastine Besilate

产品编号 T6405 CAS 190786-44-8

别名: Talion, TAU 284, 苯磺酸贝托司汀, Bepreve, Bepotastine Beslilate

Bepotastine Besilate (TAU 284) 是一种选择性可口服的组胺 H1 受体拮抗剂，可用于过敏性鼻炎、过敏性结膜炎、荨麻疹和瘙痒症的研究。

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Bepotastine Besilate, CAS 190786-44-8

规格	价格/CNY	货期
10 mg	￥ 118	现货
25 mg	￥ 178	现货
50 mg	￥ 247	现货
100 mg	￥ 413	现货
500 mg	￥ 980	现货
1 mL * 10 mM (in DMSO)	￥ 272	现货

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其他形式的 Bepotastine Besilate:

Bepotastine
现货
Bepotastine tosylate
询价

选择批次

纯度: 99.86%

纯度: 99.83%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Bepotastine Besilate (TAU 284) 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]
激酶实验	Isothermal Titration Calorimetry (ITC) of Nucelotide Binding: The titration experiments are performed using the MSC system. In each experiment, 16 aliquots of 15 μL of geldanamycin (300 μM in 1% DMSO) are injected into 1.3 mL of protein (31 μM in 20 mMTris-HCl, pH 7.5, 1 mMEDTA) at 25 °C, and the resulting data are fit after subtracting the heats of dilution. Heats of dilution are determined in separate experiments from addition of geldanamycin into buffer and buffer into protein. No evidence for binding of DMSO in the nucleotide binding site is observed. Titration data are fit using a nonlinear least-squares curve-fitting algorithm with three floating variables: stoichiometry, binding constant (Kb) 1/Kd), and change of enthalpy of interaction (ΔH°). Dissociation constants estimated for geldanamycin binding to intact yeast Hsp90 is 1.22 μM, and for binding to Hsp90 N-terminal domain is 0.78 μM. No meaningful heat is observed with binding to the C-terminal fragment.

别名	Talion, TAU 284, 苯磺酸贝托司汀, Bepreve, Bepotastine Beslilate
分子量	547.06
分子式	C21H25ClN2O3·C6H6O3S
CAS No.	190786-44-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 101 mg/mL (184.6 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.828 mL	9.1398 mL	18.2795 mL	45.6988 mL
	5 mM	0.3656 mL	1.828 mL	3.6559 mL	9.1398 mL
	10 mM	0.1828 mL	0.914 mL	1.828 mL	4.5699 mL
	20 mM	0.0914 mL	0.457 mL	0.914 mL	2.2849 mL
	50 mM	0.0366 mL	0.1828 mL	0.3656 mL	0.914 mL
	100 mM	0.0183 mL	0.0914 mL	0.1828 mL	0.457 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Da Prada M, et al. J Pharmacol Exp Ther, 1989, 248(1), 400-414. 2. Ohashi R, et al. Drug Metab Dispos, 2006, 34(5), 793-799. 3. Andoh T, et al. Eur J Pharmacol, 2006, 547(1-3), 59-64. 4. Kida T, et al. Exp Eye Res, 2010, 91(1), 85-91. 5. Tanizaki H, et al. Int Arch Allergy Immunol, 2008, 145(4), 277-282.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Bepotastine Besilate 190786-44-8 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor Inhibitor TAU-284 Bepotastine Talion inhibit pruritus TAU 284 TAU284 urticaria atopic dermatitis conjunctivitis LTB 4 苯磺酸贝托司汀 Bepreve Bepotastine Beslilate inhibitor

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Bepotastine Besilate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords