Proguanil hydrochloride
Based on 3 publication(s) in Google Scholar
Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
For research use only. We do not sell to patients.
- Purity: 99.21%
- CAS No.: 637-32-1
- Formula: C11H17Cl2N5
- Molecular Weight:290.19
-
Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Anti-Infection Compound Library
HY-L002
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
FDA-Approved Drug Library
HY-L022
-
Anti-Aging Compound Library
HY-L034
-
Drug Repurposing Compound Library
HY-L035
-
Orally Active Compound Library
HY-L061
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Antiparasitic Compound library
HY-L082
-
Anti-Cancer Metabolism Compound Library
HY-L083
-
Pediatric Drug Library
HY-L104
-
Human Metabolite Library
HY-L123
-
Off-patent Drug Library
HY-L141
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
Publications Citing Use of MedChemExpress (MCE) Proguanil hydrochloride
MoreAll Parasite Isoforms
More
Biological Activity
|
Plasmodium |
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.
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.
Chemical Information
-
CAS No. 637-32-1
-
Appearance Solid
-
Molecular Weight 290.19
-
Formula C11H17Cl2N5
-
Color White to off-white
-
SMILES
N=C(NC1=CC=C(Cl)C=C1)NC(NC(C)C)=N.[H]Cl
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
Pharmaceuticals (Basel)
2024 Sep 19;17(9):1234. PMID: 39338396 -
ACS Omega
Identification of New Modulators and Inhibitors of Palmitoyl-Protein Thioesterase 1 for CLN1 Batten Disease and Cancer. [Abstract]2024 Feb 28;9(10):11870-11882. PMID: 38496939 -
Cell Signal
Proguanil inhibits proliferation and migration in glioblastoma development through targeting CSF1R receptor. [Abstract]2024 Dec 9:111550. PMID: 39662608
Solvent & Solubility
DMSO : 125 mg/mL (430.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (272 KB)
-
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Portuguese - PT (479 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]
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4460 mL | 17.2301 mL | 34.4602 mL | 86.1505 mL |
| 5 mM | 0.6892 mL | 3.4460 mL | 6.8920 mL | 17.2301 mL | |
| 10 mM | 0.3446 mL | 1.7230 mL | 3.4460 mL | 8.6150 mL | |
| 15 mM | 0.2297 mL | 1.1487 mL | 2.2973 mL | 5.7434 mL | |
| 20 mM | 0.1723 mL | 0.8615 mL | 1.7230 mL | 4.3075 mL | |
| 25 mM | 0.1378 mL | 0.6892 mL | 1.3784 mL | 3.4460 mL | |
| 30 mM | 0.1149 mL | 0.5743 mL | 1.1487 mL | 2.8717 mL | |
| 40 mM | 0.0862 mL | 0.4308 mL | 0.8615 mL | 2.1538 mL | |
| 50 mM | 0.0689 mL | 0.3446 mL | 0.6892 mL | 1.7230 mL | |
| 60 mM | 0.0574 mL | 0.2872 mL | 0.5743 mL | 1.4358 mL | |
| 80 mM | 0.0431 mL | 0.2154 mL | 0.4308 mL | 1.0769 mL | |
| 100 mM | 0.0345 mL | 0.1723 mL | 0.3446 mL | 0.8615 mL |
Powered by Bioz