1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. Alosetron ((Z)-2-butenedioate)

Alosetron ((Z)-2-butenedioate)  (Synonyms: 马来酸阿洛司琼; GR 68755 ((Z)-2-butenedioate); GR 68755X ((Z)-2-butenedioate))

目录号: HY-70050B
产品使用指南

Alosetron (GR 68755) (Z)-2-butenedioate 是一种高效、高选择性的 5-HT3 受体 (5-HT3 receptor) 拮抗剂。Alosetron (Z)-2-butenedioate 用于肠易激综合征 (IBS) 的研究。Alosetron (Z)-2-butenedioate 阻断 5HT3 介导的豚鼠肌间和粘膜下神经元的快速去极化,IC50 在 ~55 nM。Alosetron (Z)-2-butenedioate 减轻清醒或麻醉犬直肠扩张的内脏伤害性效应。具有抗炎活性。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Alosetron Hydrochloride 通常具有更好的水溶性和稳定性。

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Alosetron ((Z)-2-butenedioate) Chemical Structure

Alosetron ((Z)-2-butenedioate) Chemical Structure

CAS No. : 122852-43-1

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Alosetron ((Z)-2-butenedioate) 的其他形式现货产品:

Other Forms of Alosetron ((Z)-2-butenedioate):

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Alosetron (GR 68755) (Z)-2-butenedioate is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron (Z)-2-butenedioate is used for the research of irritable bowel syndrome (IBS). Alosetron (Z)-2-butenedioate blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron (Z)-2-butenedioate attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects[1][2].

IC50 & Target

5-HT3 Receptor

 

体内研究
(In Vivo)

Dexamethasone and Alosetron-treated (1 mg/kg; ip; daily for 6 days) rats exhibits a significant decrease in the diarrhea index, in comparison with TNBS-control group, especially after the initial 2 days of treatment following the induction of colitis[2].

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

Clinical Trial
分子量

410.42

Formula

C21H22N4O5

CAS 号
中文名称

马来酸阿洛司琼

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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产品名称:
Alosetron ((Z)-2-butenedioate)
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