1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Autophagy
  2. Histamine Receptor Autophagy
  3. Rupatadine

Rupatadine  (Synonyms: 卢帕他定; UR-12592)

目录号: HY-13511
产品使用指南

Rupatadine (UR-12592) 是一种有效的,具有口服活性的长效 PAF/H1 受体的双抑制剂,Ki 值分别为 0.55 μM 和 0.1 μM。Rupatadine 可用于过敏性鼻炎和荨麻疹的研究。

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Rupatadine Chemical Structure

Rupatadine Chemical Structure

CAS No. : 158876-82-5

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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

Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria[1][2][3].

IC50 & Target[1]

H1 Receptor

0.1 μM (Ki)

PAF

0.55 μM (Ki)

体外研究
(In Vitro)

Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA2=9.29) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4)[1].
Rupatadine competitively inhibits PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2=6.68) and in human platelet-rich plasma (HPRP) (IC50=0.68 μM), while not affecting ADP- or arachidonic acid-induced platelet aggregation[1].
Rupatadine (0.1-30 μM) inhibits TNF-α secretion in a concentration-dependent manner, with maximum values of 92.5%[2].

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

体内研究
(In Vivo)

Rupatadine blocks histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50=1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50=113 and 9.6 μg/kg i.v.)[1].
Rupatadine potently inhibits PAF-induced mortality in mice (ID50=0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50=1.6 and 0.66 mg/kg i.v.)[1].
Rupatadine (6 mg/kg) promotes the absorption of the lesions and decreased the density of lungs[3].

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

Animal Model: Male C57BL/6J mice (18 g, 6-8 wk)[3]
Dosage: 1.5, 3, 6 mg/kg
Administration: Oral gavage once a day
Result: Markedly decreased the BLM-enhanced inflammatory scores and lung index.
Clinical Trial
分子量

415.96

Formula

C26H26ClN3

CAS 号
中文名称

卢帕他定

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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