Bepotastine - CAS:125602-71-3

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Bepotastine (Synonyms:贝托司汀；贝他斯汀；贝托斯汀；贝他司汀)

目录号 : KM13172 CAS No. : 125602-71-3 纯度 : 98%

Data Sheet 产品使用指南

Bepotastine 是一种选择性的具有口服活性的第二代组胺 H1 受体 (histamine H1 receptor) 拮抗剂。Bepotastine 可用于过敏性鼻炎，过敏性结膜炎和荨麻疹/瘙痒症的研究。

规格	价格	是否有货
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research.

体外研究

Bepotastine possesses additional anti-allergic activity including stabilization of mast cell function, inhibition of eosinophilic infiltration, inhibition of IL-5 production, and inhibition of leukotriene B4 (LTB4) and LTD4 activity.
Bepotastine significantly inhibits antigen-induced stimulation of IL-5 production in human peripheral blood mononuclear cells (PBMCs) at concentrations of 10-100 μM and the effect is enhanced when the PBMCs are pre-incubated with Bepotastine.
Leukotriene B4 increased Ca2+ concentration in cultured neutrophils, which is suppressed by Bepotastine besilate (1-100 μM). Leukotriene B4 increased Ca2+ concentration in cultured dorsal root ganglion neurons, which is also suppressed by Bepotastine besilate (100 μM).

体内研究

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 (1-10 mg/kg, oral) dose-dependently suppresses scratching induced by substance P (100 nmol/site) and leukotriene B4 (0.03 nmol/site). Bepotastine in vivo dose-dependently inhibits the acceleration of histamine-induced vascular permeability and inhibits homologous passive cutaneous anaphylaxis in guinea pig studies.
In mouse models of itching, oral Bepotastine inhibits the frequency and duration of scratching behavior.

分子式

C₂₁H₂₅N₂O₃Cl

分子量

388.89

CAS号

125602-71-3

中文名称

贝托司汀；贝他斯汀；贝托斯汀；贝他司汀

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 100 mg/mL (257.14 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5714 mL	12.8571 mL	25.7142 mL
5 mM	0.5143 mL	2.5714 mL	5.1428 mL
10 mM	0.2571 mL	1.2857 mL	2.5714 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.43 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.43 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.43 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。