| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Pyrimethamine (Malocid; Khloridin; BW 50-63; NCI-C01683; BW50-63; Daraprim; NSC 3061; Tindurin; WR-297; RP-4753) is a potent dihydrofolate reductase (DHFR) inhibitor which is used as an antimalarial and antiprotozoal drug.
| ln Vitro |
Fluconazole (FLZ) in conjunction with Pyrimethamine (Pirimecidan; 4 nM–4 μM; 24 h; LLC-MK2 cells with T. gondii) suppresses T. gondii activity for FLZ concentrations of 0, 0.05, 0.1, 0.5, 1.0, and 3.0 μM, respectively, with IC50 values of 0.23, 0.19, 0.23, 0.34, 0.14, and 0.19 μM[1].
|
|---|---|
| ln Vivo |
The combination of fluconazole and sulfadiazine with pyrimethamine (Pirimecidan; 1 mg/kg; ig; daily, for 10 d; female CF1 mice with T. gondii xenograft) enhances protection against death[1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: LLC-MK2 cells with T. gondii Tested Concentrations: 4 nM-4 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited T. gondii activity and diminished parasite proliferation index. |
| Animal Protocol |
Animal/Disease Models: Female CF1 mice (18-22 g ; 4-6 week of age) with T. gondii xenograft[1]
Doses: po (oral gavage); daily, for 10 days Route of Administration: 1 mg/kg; 10 mg/kg (Fluconazole ), 40 mg/kg (Sulfadiazine) Experimental Results: Increased mouse survival compared to treatment with SDZ/PYR alone. |
| References |
[1]. Aikawa M, et, al. Studies on nuclear division of a malarial parasite under pyrimethamine treatment. J Cell Biol. 1968 Dec;39(3):749-54.
[2]. Martins-Duarte ÉS, et, al. Toxoplasma gondii: the effect of fluconazole combined with sulfadiazine and pyrimethamine against acute toxoplasmosis in murine model. Exp Parasitol. 2013 Mar;133(3):294-9. |
| Molecular Formula |
C12H13CLN4
|
|
|---|---|---|
| Molecular Weight |
248.71
|
|
| CAS # |
58-14-0
|
|
| Related CAS # |
Pyrimethamine-d3;1189936-99-9
|
|
| SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])C1C(N([H])[H])=NC(N([H])[H])=NC=1C([H])([H])C([H])([H])[H]
|
|
| InChi Key |
WKSAUQYGYAYLPV-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C12H13ClN4/c1-2-9-10(11(14)17-12(15)16-9)7-3-5-8(13)6-4-7/h3-6H,2H2,1H3,(H4,14,15,16,17)
|
|
| Chemical Name |
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
|
|
| Synonyms |
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.05 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 25.0 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: ≥ 2.5 mg/mL (10.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0207 mL | 20.1037 mL | 40.2075 mL | |
| 5 mM | 0.8041 mL | 4.0207 mL | 8.0415 mL | |
| 10 mM | 0.4021 mL | 2.0104 mL | 4.0207 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05678348 | Recruiting | Drug: Pyrimethamine | Head and Neck Cancer Cancer of the Head and Neck |
Washington University School of Medicine |
August 3, 2023 | Early Phase 1 |
| NCT05497063 | Not yet recruiting | Drug: G-COSPE® tablets | Bioequivalence | Emzor Pharmaceutical Industries Limited |
December 2022 | Phase 1 |
| NCT03057990 | Withdrawn | Drug: Pyrimethamine | Myelodysplastic Syndromes | Montefiore Medical Center | September 11, 2019 | Phase 1 |
| NCT01102686 | Completed | Drug: Pyrimethamine Drug: Leucovorin |
Gangliosidoses, GM2 Sandhoff Disease |
The Hospital for Sick Children | August 2009 | Phase 1 Phase 2 |
 |
|---|
 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
