1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Bepotastine tosylate

Bepotastine tosylate  (Synonyms: 甲苯磺酸贝托司汀;甲苯磺酸贝他斯汀;甲苯磺酸贝托斯汀;甲苯磺酸贝他司汀)

目录号: HY-I0021A
产品使用指南

Bepotastine tosylate 是一种具有选择性和口服活性的第二代组胺 H1 受体 (histamine H1 receptor) 拮抗剂,可抑制组胺介导的神经生长因子 (NGF) 表达上调。Bepotastine tosylate 可用于过敏性鼻炎,过敏性结膜炎和荨麻疹/瘙痒症的研究。

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Bepotastine tosylate Chemical Structure

Bepotastine tosylate Chemical Structure

CAS No. : 1160415-45-1

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate can suppress the expression of nerve growth factor (NGF). Bepotastine tosylate can be used in studies of allergic rhinitis, allergic conjunctivitis and urticaria/pruritus[1][2][3][4].

IC50 & Target

Histamine H1 Receptor[1][2][3][4].

体外研究
(In Vitro)

Bepotastine tosylate (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[1].
Bepotastine tosylate (50 µM; 1 h) suppresses the expression of NGF mRNA in NHEKs[2].

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

Cell Viability Assay[1]

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

Western Blot Analysis[2]

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

Bepotastine tosylate (10 g/L; eye drop; 3 times at intervals of 20 min in one eye) demonstrates significant inhibition of PAF-induced conjunctival eosinophil infiltration[1].
Bepotastine tosylate (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[3].
Bepotastine tosylate (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[3].

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

Animal Model: Guinea pigs (6-week-old)[1].
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[3].
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.
Clinical Trial
分子量

561.09

Formula

C28H33ClN2O6S

CAS 号
中文名称

甲苯磺酸贝托司汀;甲苯磺酸贝他斯汀;甲苯磺酸贝托斯汀;甲苯磺酸贝他司汀

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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