1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. Phenylbiguanide hydrochloride

Phenylbiguanide hydrochloride  (Synonyms: 苯基双胍盐酸盐; N-Phenylbiguanide hydrochloride; PBG hydrochloride; 1-Phenylbiguanide hydrochloride)

目录号: HY-101331A
产品使用指南 技术支持

Phenylbiguanide hydrochloride 是一种选择性的 5-HT3 受体激动剂,EC50 为 3.0±0.1 μM。

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Phenylbiguanide hydrochloride Chemical Structure

Phenylbiguanide hydrochloride Chemical Structure

CAS No. : 55-57-2

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Other Forms of Phenylbiguanide hydrochloride:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Phenylbiguanide hydrochloride is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.

IC50 & Target[1]

5-HT3 Receptor

3 μM (EC50)

体外研究
(In Vitro)

Phenylbiguanide (1-Phenylbiguanide) is a 5-HT3 receptor selective agonist with pEC50s of 5.57, 4.07, and 4.47 for r5-HT3A(b), h5-HT3A, m5-HT3A(b) , respectively[1]. The effect of Phenylbiguanide (1-Phenylbiguanide hydrochloride) in promoting the growth of the HT29 cell line is investigated. Phenylbiguanide causes a dose dependent proliferation of HT29 cells after 48 hours incubation. The maximum proliferation is at a 5HT concentration of 12.5 μM (P≤0.01). Phenylbiguanide significantly stimulates the growth of cells at concentrations of 3.125 μM (P≤0.05) and 6.25 μM (P≤0.01)[2].

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

体内研究
(In Vivo)

In anaesthetised mice, Phenylbiguanide (PBG), a drug that is known to stimulate cardiopulmonary afferent C-fibres,is injected into the right atrium of the heart and mapped c-Fos expression within specific regions of the central nervous system. Intraatrial injection of PBG produces a reflex cardiorespiratory response including a pronounced bradycardia and a respiratory depression[3].

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

分子量

213.67

Formula

C8H12ClN5

CAS 号
性状

固体

颜色

White to off-white

中文名称

苯基双胍盐酸盐;1-苯基双胍盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
纯度 & 产品资料
参考文献
Cell Assay
[2]

HT29 cells are washed with Phosphate buffer saline (PBS) and harvested with a 0.5% trypsin solution at 50-60% confluency. Cells are then added to wells at a density of 104 cells/well in a 96-well plate to a final volume of 100 μL/well. After 24 hours of incubation at 37°C in a 5% CO2 atmosphere, the culture medium is replaced with 200 μL fresh culture medium containing 5HT hydrochloride, Phenylbiguanide hydrochloride at concentrations of: 3.125, 6.25, 12.5, 25, 50, and 100 µM . Cells cultured solely in media served as negative controls. After 48 hours of incubation at 37°C in a 5% CO2 atmosphere, the culture medium is removed and 8 µL MTT reagent (diluted in PBS at a concentration of 4 mg/mL) is added to 50 μL of fresh culture medium at a final concentration of 0.55 mg/mL. The optimum incubation period time is determined in a pilot study[2].

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

Animal Administration
[3]

Mice[3]
Adult male specified pathogen free (SPF) BALB/c mice (28-33 g; n=10) are used throughout this study. All mice have free access to water and food in a light (12: 12 h light/ dark cycle, lights on at 0700 h) and temperature-controlled (21-23°C) environment. Mice are randomly assigned to two treatment groups, 1) intra-atrial injection of 0.9% saline (controls, n=5) or 2) intra-atrial injection of vehicle containing Phenylbiguanide (n=5). For the PBGinjected group, mice are injected with an effective dose of Phenylbiguanide (1-1.5 μg in 10-15 μL saline) . This is repeated five times in total with each injection separated by 8-10 min. For control mice, each mouse receives five saline injections (10-15 μL each), also at 8-10 min intervals[3].

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

参考文献

Phenylbiguanide hydrochloride 相关分类

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  • 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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