| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Cycloguanil targets dihydrofolate reductase (DHFR), an enzyme essential for the synthesis of tetrahydrofolate, a cofactor required for DNA synthesis. By inhibiting DHFR, cycloguanil depletes tetrahydrofolate levels, leading to reduced synthesis of thymidylate and purines, and ultimately inhibiting DNA replication and cell division in Plasmodium parasites.
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| ln Vitro |
In vitro, cycloguanil is a DHFR inhibitor with antimalarial activity against Plasmodium parasites. Its activity is assessed by measuring DHFR inhibition in enzyme assays and by assessing parasite growth inhibition in cell-based assays. The compound is the active metabolite of the antimalarial drug proguanil.
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| ln Vivo |
In vivo, cycloguanil is formed as a metabolite of proguanil and is responsible for the antimalarial activity of the parent drug. It is used in combination with other antimalarial agents such as atovaquone for the treatment of Plasmodium infections. The compound's DHFR inhibition leads to parasite death and clearance of infection.
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| Enzyme Assay |
In vitro enzyme assays for cycloguanil measure its inhibition of DHFR activity. The enzyme is incubated with dihydrofolate substrate and NADPH in the presence of varying concentrations of the compound. The production of tetrahydrofolate is measured spectrophotometrically or by HPLC. IC50 values are calculated from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for cycloguanil use Plasmodium parasite cultures to assess antimalarial activity. Parasites are cultured in appropriate media and exposed to serial dilutions of the compound. Parasite growth inhibition is measured by assessing parasite viability or by quantifying parasite DNA. EC50 values are determined from dose-response curves.
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| Animal Protocol |
In vivo animal models for cycloguanil include mouse models of malaria infection. Animals are infected with Plasmodium parasites and treated with cycloguanil or proguanil at various doses. Efficacy is evaluated by measuring parasitemia, survival rates, and clinical signs of infection. Pharmacokinetic studies measure drug exposure and metabolite formation.
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| ADME/Pharmacokinetics |
Cycloguanil HCl has a molecular formula of C11H15Cl2N5 and a molecular weight of 288.18 g/mol. It is also known as Cycloguanil hydrochloride and has the IUPAC name 1-(4-chlorophenyl)-6,6-dimethyl-1,3,5-triazine-2,4-diamine;hydrochloride. The compound has a purity of ≥98% and is stored under appropriate conditions for research use.
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| Toxicity/Toxicokinetics |
The toxicity profile of cycloguanil includes the potential for adverse effects associated with DHFR inhibition, including folate depletion and hematological toxicity. The compound is for research use only and is not approved for clinical use as a single agent. Appropriate safety precautions should be taken during handling.
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| References |
: Le Bras J, Basco LK, Cremer G, Charmot G. [Contribution of molecular genetics to the understanding of chemoresistance of Plasmodium falciparum]. Bull Soc Pathol Exot. 1992;85(2):146-9. Review. French. PubMed PMID: 1356539.
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| Additional Infomation |
Cycloguanil hydrochloride is the hydrochloride salt of cyclic guanidine. It is an organic molecular entity belonging to the hydrochloride salt category. It contains cyclic guanidine molecules.
Cycloguanil HCl is the hydrochloride salt of cycloguanil, an active metabolite of the antimalarial drug proguanil. It is a dihydrofolate reductase (DHFR) inhibitor and is used as an antimalarial agent in combination with other drugs such as atovaquone. Cycloguanil is also known as Cycloguanil hydrochloride and is intended for laboratory research use only. |
| Molecular Formula |
C11H15CL2N5
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|---|---|
| Molecular Weight |
288.1763
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| Exact Mass |
287.07
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| CAS # |
152-53-4
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| Related CAS # |
Cycloguanil;516-21-2;Cycloguanil-d4 hydrochloride;1189427-23-3
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| PubChem CID |
9048
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| Appearance |
White to off-white solid powder
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| Boiling Point |
400.7ºC at 760mmHg
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| Melting Point |
210-215ºC
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| Flash Point |
196.1ºC
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| Vapour Pressure |
1.25E-06mmHg at 25°C
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| LogP |
2.664
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
355
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MOUAPRKJJUXEIE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H14ClN5.ClH/c1-11(2)16-9(13)15-10(14)17(11)8-5-3-7(12)4-6-8;/h3-6H,1-2H3,(H4,13,14,15,16);1H
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| Chemical Name |
1-(4-chlorophenyl)-6,6-dimethyl-1,3,5-triazine-2,4-diamine;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~216.88 mM)
H2O : ~25 mg/mL (~86.75 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4701 mL | 17.3503 mL | 34.7005 mL | |
| 5 mM | 0.6940 mL | 3.4701 mL | 6.9401 mL | |
| 10 mM | 0.3470 mL | 1.7350 mL | 3.4701 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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