Phenylbiguanide (Synonyms: N-Phenylbiguanide; PBG; 1-Phenylbiguanide)

Cat. No.: HY-101331 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

For research use only. We do not sell to patients.

Phenylbiguanide Chemical Structure

CAS No. : 102-02-3

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Protocol
Purity & Documentation
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Description

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

IC₅₀ & Target

EC50: 3.0±0.1 μM (5-HT₃ Receptor)^[1]

In Vitro

Phenylbiguanide (1-Phenylbiguanide) is a 5-HT₃ receptor selective agonist with pEC₅₀s of 5.57, 4.07, and 4.47 for r5-HT_3A(b), h5-HT_3A, m5-HT_3A(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].

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

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].

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

Molecular Weight

177.21

Formula

C₈H₁₁N₅

CAS No.

102-02-3

Appearance

Solid

Color

White to off-white

SMILES

NC(NC(NC1=CC=CC=C1)=N)=N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 150 mg/mL (846.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 25 mg/mL (141.08 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	5.6430 mL	28.2151 mL	56.4302 mL
5 mM	1.1286 mL	5.6430 mL	11.2860 mL
10 mM	0.5643 mL	2.8215 mL	5.6430 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (14.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (14.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (14.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (247 KB) SDS (0 KB)

COA (244 KB) HNMR (236 KB)

Handling Instructions (2659 KB)

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	5.6430 mL	28.2151 mL	56.4302 mL	141.0756 mL
	5 mM	1.1286 mL	5.6430 mL	11.2860 mL	28.2151 mL
	10 mM	0.5643 mL	2.8215 mL	5.6430 mL	14.1076 mL
	15 mM	0.3762 mL	1.8810 mL	3.7620 mL	9.4050 mL
	20 mM	0.2822 mL	1.4108 mL	2.8215 mL	7.0538 mL
	25 mM	0.2257 mL	1.1286 mL	2.2572 mL	5.6430 mL
	30 mM	0.1881 mL	0.9405 mL	1.8810 mL	4.7025 mL
	40 mM	0.1411 mL	0.7054 mL	1.4108 mL	3.5269 mL
	50 mM	0.1129 mL	0.5643 mL	1.1286 mL	2.8215 mL
	60 mM	0.0941 mL	0.4703 mL	0.9405 mL	2.3513 mL
	80 mM	0.0705 mL	0.3527 mL	0.7054 mL	1.7634 mL
	100 mM	0.0564 mL	0.2822 mL	0.5643 mL	1.4108 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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.

Keywords:

Phenylbiguanide102-02-3N-Phenylbiguanide PBG 1-PhenylbiguanideInhibitorinhibitorinhibit

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