Phenylbiguanide-N-Phenylbiguanide-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPhenylbiguanideCat. No.: HY-101331CAS No.: 102-02-3Synonyms: N-Phenylbiguanide; PBG; 1-Phenylbiguanide分式: CHN分量: 177.21作靶點(diǎn): 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6

2、months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 150 mg/mL (846.45 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 5.6430 mL 28.2151 mL 56.4302 mL5 mM 1.1286 mL 5.6430 mL 11.2860 mL10 mM 0.5643 mL 2.8215 mL 5.6430 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先

3、配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (14.11 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (14.11 mM); Clear solution3.

4、請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (14.11 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Phenylbiguanide種選擇性的 5-HT3 受體激動(dòng)劑，EC50 為 3.00.1 M。IC50 & Target 5-HT3 Receptor3 M (EC50)體外研究 Phenylbiguanide (1-Phenylbiguanide) is a 5-HT3 receptor

5、selective agonist with pEC50s of 5.57, 4.07, and4.47 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

6、 after 48 hours incubation. Themaximum proliferation is at a 5HT concentration of 12.5 M (P0.01). Phenylbiguanide significantlystimulates the growth of cells at concentrations of 3.125 M (P0.05) and 6.25 M (P0.01) 2.體內(nèi)研究 In anaesthetised mice, Phenylbiguanide (PBG), a drug that is known to stimulate

7、 cardiopulmonary afferent C-fibres,is injected into the right atrium of the heart and mapped c-Fos expression within specific regions of thecentral nervous system. Intraatrial injection of PBG produces a reflex cardiorespiratory response including apronounced bradycardia and a respiratory depression

8、 3.PROTOCOLCell 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 finalvolume of 100 L/well. After 24 hours of incubation at 37C in a 5

9、% CO2 atmosphere, the culture medium isreplaced with 200 L fresh culture medium containing 5HT hydrochloride, Phenylbiguanide hydrochloride atconcentrations of: 3.125, 6.25, 12.5, 25, 50, and 100 M . Cells cultured solely in media served as negativecontrols. After 48 hours of incubation at 37C in a

10、5% CO2 atmosphere, the culture medium is removed and8 L MTT reagent (diluted in PBS at a concentration of 4 mg/mL) is added to 50 L of fresh culture mediumat 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 t

11、he accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 Adult male specified pathogen free (SPF) BALB/c mice (28-33 g; n=10) are used throughout this study. Allmice have free access to water and food in a light (12: 12 h light/ dark cycle, lights on at 0700 h) andtemp

12、erature-controlled (21-23C) 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 Phenyl

13、biguanide (1-1.5 g in10-15 L saline) . This is repeated five times in total with each injection separated by 8-10 min. For controlmice, each mouse receives five saline injections (10-15 L each), also at 8-10 min intervals 3.MCE has not independently confirmed the accuracy of these methods. They are

14、for reference only.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEREFERENCES1. Mair ID, et al. Pharmacological characterization of a rat 5-hydroxytryptamine type3 receptor subunit (r5-HT3A(b) expressed in Xenopuslaevis oocytes. Br J Pharmacol. 1998 Aug;124(8):1667-74.2. Ataee R, et al. Study of 5H

15、T3 and HT4 receptor expression in HT29 cell line and human colon adenocarcinoma tissues. Arch Iran Med.2010 Mar;13(2):120-5.3. de Vries A, et al. Characterisation of c-Fos expression in the central nervous system of mice following right atrialinjections of the 5-HT3receptor agonist Phenylbiguanide. Auton Neurosci. 20