Proguanil

Name: Proguanil
Brand: MedChemExpress
SKU: HY-B0806
Rating: 4.5 (1 reviews)

Cat. No.: HY-B0806 Purity: 99.84%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.

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

Proguanil Chemical Structure

CAS No. : 500-92-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 145	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 238	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Proguanil:

1 Publications Citing Use of MCE Proguanil

•ACS Omega. 2024 Feb 28;9(10):11870-11882. [Abstract]

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor^[1]^[2].

IC₅₀ & Target

Plasmodium

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	13 μM Compound: Proguanil	Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31864776]
A549	IC₅₀	3.8 μM Compound: Proguanil	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31864776]
HCT-116	IC₅₀	8.4 μM Compound: Proguanil	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31864776]
HEK293	EC₅₀	> 10000 nM Compound: BIG22	Agonist activity at human TAAR1 expressed in HEK293 cells assessed as cAMP accumulation after 20 mins by BRET assay Agonist activity at human TAAR1 expressed in HEK293 cells assessed as cAMP accumulation after 20 mins by BRET assay	[PMID: 27823885]
HeLa	EC₅₀	> 100 μM Compound: 30	Antiviral activity against Respiratory syncytial virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against Respiratory syncytial virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
HeLa	EC₅₀	> 100 μM Compound: 30	Antiviral activity against coxsackie B4 virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against coxsackie B4 virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
HeLa	EC₅₀	> 100 μM Compound: 30	Antiviral activity against vesicular stomatitis virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against vesicular stomatitis virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
MDCK	CC₅₀	> 100 μM Compound: 30	Cytotoxicity against dog MDCK cells assessed as reduction in cell viability measured after 5 to 6 days by MTS assay Cytotoxicity against dog MDCK cells assessed as reduction in cell viability measured after 5 to 6 days by MTS assay	[PMID: 28477572]
T-24	IC₅₀	18.4 μM Compound: Proguanil	Antiproliferative activity against human T24 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human T24 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31864776]
UMUC3	IC₅₀	16.3 μM Compound: Proguanil	Antiproliferative activity against human UM-UC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human UM-UC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31864776]

In Vitro

Proguanil per se has only weak antimalarial activity in vitro (IC₅₀=2.4-19 μM), and its effectiveness depends on the active metabolite Cycloguanil (IC₅₀=0.5-2.5 nM). The Cycloguanil is a dihydrofolate reductase (DHFR) inhibitor. The combination of Atovaquone and Proguanil is synergistic in vitro. Both drugs also have activity against gametocytes and pre-erythrocytic (hepatic) stages of malaria parasites^[1].
Proguanil acts as a biguanide rather than as its metabolite Cycloguanil (a parasite dihydrofolate reductase [DHFR] inhibitor) to enhance the Atovaquone effect. Proguanil-mediated enhancement is specific for Atovaquone, since the effects of other mitochondrial electron transport inhibitors, such as Myxothiazole and Antimycin, are not altered by inclusion of Proguanil^[2].
5-HT₃ receptor responses are reversibly inhibited by Proguanil, the metabolite 4-chlorophenyl-1-biguanide (CPB) and the active metabolite Cycloguanil (CG), with an IC₅₀ of 1.81, 1.48 and 4.36 μM, respectively^[3].

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

In Vivo

Proguanil (p.o.; 2.9 mg/kg body weight; daily for 5 days and 6 weeks respectively) shows mild degenerative changes for five days, while shows severe degenerative changes for six weeks in wistar strain albino rats^[4].
Serum testosterone level is significantly decreased for proguanil treatment rats^[4].
Administration of Malarone (atovaquone and proguanil) to experimentally B. gibsoni infected two dogs in chronic stage and three dogs in acute stage results in decrease in parasitemia, and clinical improvements are observed^[5].

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

Clinical Trial

Molecular Weight

253.73

Formula

C₁₁H₁₆ClN₅

CAS No.

500-92-5

Appearance

Solid

Color

White to off-white

SMILES

N=C(NC1=CC=C(Cl)C=C1)NC(NC(C)C)=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 : ≥ 130 mg/mL (512.36 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.9412 mL	19.7060 mL	39.4120 mL
5 mM	0.7882 mL	3.9412 mL	7.8824 mL
10 mM	0.3941 mL	1.9706 mL	3.9412 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.

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.17 mg/mL (8.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (8.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (8.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 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 (21.7 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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.84%

Select Batch:

Data Sheet (275 KB) SDS (392 KB)

COA (243 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Pudney M, et al. Atovaquone and proguanil hydrochloride: a review of nonclinical studies. J Travel Med. 1999 May;6 Suppl 1:S8-12. [Content Brief]

[2]. Srivastava IK, et al. A mechanism for the synergistic antimalarial action of atovaquone and proguanil. Antimicrob Agents Chemother. 1999 Jun;43(6):1334-9. [Content Brief]

[3]. Lochner M, et al. The antimalarial drug proguanil is an antagonist at 5-HT3 receptors. J Pharmacol Exp Ther. 2014 Dec;351(3):674-84. [Content Brief]

[4]. Stephen AO, et al. Prolonged administration of proguanil induces reproductive toxicity in male rats. J Toxicol Sci. 2011 Oct;36(5):587-99. [Content Brief]

[5]. Iguchi A, et al. The in vitro interactions and in vivo efficacy of atovaquone and proguanil against Babesia gibsoni infection in dogs. Vet Parasitol. 2013 Nov 8;197(3-4):527-33. [Content Brief]

Cell Assay ^[4]	Sertoli cells obtained from sixteen to eighteen day-old-rats are cultured and treated with 0.3 μM to 10 μM of proguanil for 5 days after which Sertoli cell viability and nuclei integrity are determined. Also, the genetic expressions of transferrin and Glial cell line-derived neurotrophic factor are assessed^[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[4]	Rats: Groups of ten to twelve-week-old rats are administered proguanil (2.9 mg/kg body weight) daily for 5 days and 6 weeks respectively. Thereafter, body and reproductive organ weights are taken, sperm parameters are analyzed, while the histology of the testis and epididymis are carried out. Also, serum levels of testosterone, luteinizing hormone and follicle stimulating hormone are determined^[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Pudney M, et al. Atovaquone and proguanil hydrochloride: a review of nonclinical studies. J Travel Med. 1999 May;6 Suppl 1:S8-12. [Content Brief] [2]. Srivastava IK, et al. A mechanism for the synergistic antimalarial action of atovaquone and proguanil. Antimicrob Agents Chemother. 1999 Jun;43(6):1334-9. [Content Brief] [3]. Lochner M, et al. The antimalarial drug proguanil is an antagonist at 5-HT3 receptors. J Pharmacol Exp Ther. 2014 Dec;351(3):674-84. [Content Brief] [4]. Stephen AO, et al. Prolonged administration of proguanil induces reproductive toxicity in male rats. J Toxicol Sci. 2011 Oct;36(5):587-99. [Content Brief] [5]. Iguchi A, et al. The in vitro interactions and in vivo efficacy of atovaquone and proguanil against Babesia gibsoni infection in dogs. Vet Parasitol. 2013 Nov 8;197(3-4):527-33. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.9412 mL	19.7060 mL	39.4120 mL	98.5299 mL
	5 mM	0.7882 mL	3.9412 mL	7.8824 mL	19.7060 mL
	10 mM	0.3941 mL	1.9706 mL	3.9412 mL	9.8530 mL
	15 mM	0.2627 mL	1.3137 mL	2.6275 mL	6.5687 mL
	20 mM	0.1971 mL	0.9853 mL	1.9706 mL	4.9265 mL
	25 mM	0.1576 mL	0.7882 mL	1.5765 mL	3.9412 mL
	30 mM	0.1314 mL	0.6569 mL	1.3137 mL	3.2843 mL
	40 mM	0.0985 mL	0.4926 mL	0.9853 mL	2.4632 mL
	50 mM	0.0788 mL	0.3941 mL	0.7882 mL	1.9706 mL
	60 mM	0.0657 mL	0.3284 mL	0.6569 mL	1.6422 mL
	80 mM	0.0493 mL	0.2463 mL	0.4926 mL	1.2316 mL
	100 mM	0.0394 mL	0.1971 mL	0.3941 mL	0.9853 mL

Proguanil Related Classifications

Infection

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:

Proguanil500-92-5ParasiteAntifolateantimalarialinfectionembryotoxicitytoxicitybiguanidereproductiveInhibitorinhibitorinhibit

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Proguanil

Customer Review

Other Forms of Proguanil:

Proguanil Related Antibodies

1 Publications Citing Use of MCE Proguanil

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View All Parasite Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Proguanil Related Antibodies

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Complete Stock Solution Preparation Table

Proguanil Related Classifications

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