Cycloguanil-d6 (hydrochloride) (Synonyms: Chloroguanide Triazine-d6) |
| Katalog-Nr.GC47142 |
A neuropeptide with diverse biological activities
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2712364-69-5
Sample solution is provided at 25 µL, 10mM.
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Cycloguanil-d6 is intended for use as an internal standard for the quantification of cycloguanil by GC- or LC-MS. Cycloguanil is the active metabolite of the antimalarial prodrug proguanil.1 Cycloguanil is formed from proguanil by the cytochrome P450 (CYP) isoforms CYP2C19 and CYP3A in human liver microsomes. It is an inhibitor of dihydrofolate reductase (DHFR; Kis = 1.5 and 0.79 nM for the P. falciparum and P. berghei enzymes, respectively).2,3 It is active against ten P. falciparum field isolates (IC50s = 0.12-1,400 µg/ml).2 Cycloguanil reduces parasitemia in a mouse model of P. berghei infection (ED50 = 2 mg/kg).4 It also reduces parasitemia in a rhesus monkey model of P. cynomolgi infection when administered at a dose of 0.3 mg/kg.5
1.Birkett, D.J., Rees, D., Anderson, T., et al.In vitro proguanil activation to cycloguanil by human liver microsomes is mediated by CYP3A isoforms as well as by S-mephenytoin hydroxylaseBr. J. Clin. Pharmacol.37(5)413-420(1994) 2.Foote, S.J., Galatis, D., and Cowman, A.F.Amino acids in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum involved in cycloguanil resistance differ from those involved in pyrimethamine resistanceProc. Natl. Acad. Sci. USA87(8)3014-3017(1990) 3.Yuthavong, Y., Vilaivan, T., Chareonsethakul, N., et al.Development of a lead inhibitor for the A16V+S108T mutant of dihydrofolate reductase from the cycloguanil-resistant strain (T9/94) of Plasmodium falciparumJ. Med. Chem.43(14)2738-2744(2000) 4.Knight, D.J., and Peters, W.The antimalarial activity of N-benzyloxydihydrotriazines. I. The activity of clociguanil (BRL 50216) against rodent malaria, and studies on its mode of actionAnn. Trop. Med. Parasitol.74(4)393-404(1980) 5.Schmidt, L.H., Loo, T.L., Fradkin, R., et al.Antimalarial activities of triazine metabolites of chlorguanide and dichlorguanideProc. Soc. Exp. Biol. Med.80(2)367-370(1952)
| Cas No. | 2712364-69-5 | SDF | |
| Überlieferungen | Chloroguanide Triazine-d6 | ||
| Canonical SMILES | ClC1=CC=C(N2C(N)=NC(N)=NC2(C([2H])([2H])[2H])C([2H])([2H])[2H])C=C1.Cl | ||
| Formula | C11H8ClD6N5.HCl | M.Wt | 294.2 |
| Löslichkeit | DMSO: soluble | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.399 mL | 16.9952 mL | 33.9905 mL |
| 5 mM | 0.6798 mL | 3.399 mL | 6.7981 mL |
| 10 mM | 0.3399 mL | 1.6995 mL | 3.399 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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