Bepotastine Besilate|190786-44-8|(苯磺酸贝托司汀)-陌孚医药/Medlife

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Bepotastine Besilate (Synonyms: 苯磺酸贝托司汀)

目录号: PC14215 纯度: ≥98%

CAS No. :190786-44-8

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PC14215-200mg	200mg	¥3430.00	请登录
PC14215-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥490.00	请登录

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中文名称	Bepotastine Besilate
中文别名	苯磺酸贝托司汀;N,N,N-三甲基-4-十二烷基苯甲基氯化铵;苯磺贝他斯汀;苯磺酸贝他斯汀;苯磺酸贝托斯汀;苯磺酸倍他司汀;苯磺酸贝他司汀;苯磺酸贝托斯汀及中间体;(+)-(S)-4-{4-[(4-氯苯基)(2-吡啶)甲氧基]哌啶}丁酸苯磺酸盐
英文名称	Bepotastine Besilate
英文别名	Bepotastine besilate;(+)-(S)-4-[4-[1-(4-Chlorophenyl)-1-(2-pyridyl)methoxy]piperidin-1-yl]butyric acid benzenesulfonate;1-Piperidinebutanoic acid, 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-, benzenesulfonate;benzenesulfonic acid,4-[4-[(S)-(4-chlorophenyl)-pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid;Bepotastine (Beslilate);Bepotastine Besylate;Bepotastine benzenesulfonate;Bepreve;Betotastine besilate;Talion;TAU-284;UNII-6W18MO1QR3;TAU 284;Talion (TN);Bepotastine Beslilat;Bepotastine Beslilate;Benzenesulfonate salt;Bepotastine besylate [USAN];6W18MO1QR3;4-((4-Chlorophenyl)-2-pyridinylmethoxy)- (S)-1-piperidinebutanoic acid monobenzenesulfonate;(+)-(S)-4-(4-((4-Chlorophenyl)(2-pyridyl)methoxy)piperidino)butyric acid monobenzenesulfonate;4-{4-[(s)-(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidin-1-yl}buta
Cas No.	190786-44-8
分子式	C₂₇H₃₁ClN₂O₆S
分子量	547.06
包装储存	Sealed and stored at 4℃，, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research.

性状

Solid

IC50 & Target[1][2]

Histamine H1 receptor.

体外研究(In Vitro)

Bepotastine besilate (10, 100, 1000 μM; preincubates for 120 min) decreases the release of histamine induced by A23187 treatment, which reaches a statistically significant reduces level at 1000 μM.
Bepotastine besilate (50 μM; 1 h) suppresses the expression of NGF mRNA in NHEKs.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	NHEKs
Concentration:	50 μM (preincubation)
Incubation Time:	1 h
Result:	Suppressed the expression of NGF mRNA in NHEKs.

Western Blot Analysis

Cell Line:	RPMCs
Concentration:	10, 100, 1000 μM
Incubation Time:	120 min (preincubate)
Result:	Decreased the release of histamine.

体内研究(In Vivo)

Bepotastine besilate (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) demonstrates significant inhibition of PAF-induced conjunctival eosinophil infiltration.
Bepotastine besilate (3 mg/kg; p.o.; once) suppresses scratching behavior to a frequency of 59.0 and a duration of 14.57 seconds, which are almost the same levels compares with the control.
Bepotastine besilate (10 mg/kg; p.o.; once) significantly suppresses serum LTB 4 levels to 711.3 pg/mL at 1 h and 858.8 pg/mL at 2 h in NC/Nga mice with a rash.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Guinea pigs (6-week-old).
Dosage:	10 g/L (1.0% (w/v)) for 10 μL.
Administration:	Eye drop; 3 times at intervals of 20 min (in one eye).
Result:	Inhibited PAF-induced conjunctival eosinophil infiltration.

Animal Model:	Male BALB/c mice(12-week-old); NC/Nga mice.
Dosage:	3, 10 mg/kg
Administration:	Oral administration; once (1 h before induces scratching behavior of Male BALB/c mice).
Result:	Significantly inhibited histamine-mediated scratching behavior in male BALB/c mice. Significantly suppressed serum LTB 4 levels in NC/Nga mice with a rash.

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃，, away from moisture

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

ClinicalTrial

参考文献

[1]. Kida T, et al. Bepotastine besilate, a highly selective histamine H(1) receptor antagonist, suppresses vascular hyperpermeability and eosinophil recruitment in 体外研究 and in vivo experimental allergic conjunctivitis models. Exp Eye Res. 2010 Jul;91(1):8 [Information]

[2]. Kamata Y, et al. Bepotastine besilate downregulates the expression of nerve elongation factors in normal human epidermal keratinocytes. J Dermatol Sci. 2018 Apr 23:S0923-1811(18)30186-5. [Information]

[3]. Tanizaki H, et al. Oral administration of bepotastine besilate suppressed scratching behavior of atopic dermatitis model NC/Nga mice. Int Arch Allergy Immunol. 2008;145(4):277-82. [Information]

[4]. Jon I Williams, et al. Non-clinical pharmacology, pharmacokinetics, and safety findings for the antihistamine bepotastine besilate. Curr Med Res Opin. 2010 Oct;26(10):2329-38. [Information]

溶解度数据

体外研究:

DMSO : ≥ 100 mg/mL (182.80 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8280 mL	9.1398 mL	18.2795 mL
5 mM	0.3656 mL	1.8280 mL	3.6559 mL
10 mM	0.1828 mL	0.9140 mL	1.8280 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.57 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.57 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.57 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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