2. Cell Cycle/DNA Damage Anti-infection
  3. Antifolate Parasite
  4. Pyrimethamine

Pyrimethamine  (Synonyms: Pirimecidan; Pirimetamin; RP 4753)

Cat. No.: HY-18062 Purity: 99.83%
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Pyrimethamine (Pirimecidan) is a potent, orally active dihydrofolate reductase (DHFR) inhibitor. Pyrimethamine is an antimalarial agent. Pyrimethamine affects the nucleoprotein metabolism of malarial parasites by interference in the folic–folinic acid systems and affects cell division by inhibiting the conversion of dihydrofolate to tetrahydrofolate.

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

Pyrimethamine Chemical Structure

Pyrimethamine Chemical Structure

CAS No. : 58-14-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 87 In-stock
Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Solid
100 mg USD 79 In-stock
500 mg USD 185 In-stock
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5 g   Get quote  

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Based on 7 publication(s) in Google Scholar

Other Forms of Pyrimethamine:

Pyrimethamine Related Antibodies

Top Publications Citing Use of Products

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Pyrimethamine (Pirimecidan) is a potent, orally active dihydrofolate reductase (DHFR) inhibitor. Pyrimethamine is an antimalarial agent. Pyrimethamine affects the nucleoprotein metabolism of malarial parasites by interference in the folic–folinic acid systems and affects cell division by inhibiting the conversion of dihydrofolate to tetrahydrofolate[1][2].

IC50 & Target

Plasmodium

 

In Vitro

Pyrimethamine (Pirimecidan; 4 nM-4 μM; 24 h; LLC-MK2 cells with T. gondii) combination of Fluconazole (FLZ) (HY-B0101) inhibits T. gondii activity with IC50 values of 0.23, 0.19, 0.23, 0.34, 0.14, and 0.19 μM for FLZ concentration at 0, 0.05, 0.1, 0.5, 1.0, and 3.0 μM, respectively[1].

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

Pyrimethamine Related Antibodies

Cell Viability Assay[1]

Cell Line: LLC-MK2 cells with T. gondii
Concentration: 4 nM-4 μM
Incubation Time: 24 hours
Result: Inhibited T. gondii activity and decreased parasite proliferation index.
In Vivo

Pyrimethamine (Pirimecidan; 1 mg/kg; i.g.; daily, for 10 d; female CF1 mice with T. gondii xenograft) combination of Fluconazole (HY-B0101) and Sulfadiazine (HY-B0273) increases protection from death[1].

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

Animal Model: Female CF1 mice (18-22 g; 4-6 week of age) with T. gondii xenograft[1]
Dosage: Oral gavage; daily, for 10 days
Administration: 1 mg/kg; 10 mg/kg (Fluconazole (HY-B0101)), 40 mg/kg (Sulfadiazine (HY-B0273))
Result: Increased mouse survival compared to treatment with SDZ/PYR alone.
Clinical Trial
Molecular Weight

248.71

Formula

C12H13ClN4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC(N)=C(C2=CC=C(Cl)C=C2)C(CC)=N1
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 : 20 mg/mL (80.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.5 mg/mL (10.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (10.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% PBS

    Solubility: 25 mg/mL (100.52 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.90%

COA (249 KB) HNMR (166 KB) LCMS (357 KB)

Handling Instructions (2659 KB)
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.0207 mL 20.1037 mL 40.2075 mL 100.5187 mL
5 mM 0.8041 mL 4.0207 mL 8.0415 mL 20.1037 mL
10 mM 0.4021 mL 2.0104 mL 4.0207 mL 10.0519 mL
15 mM 0.2680 mL 1.3402 mL 2.6805 mL 6.7012 mL
20 mM 0.2010 mL 1.0052 mL 2.0104 mL 5.0259 mL
25 mM 0.1608 mL 0.8041 mL 1.6083 mL 4.0207 mL
30 mM 0.1340 mL 0.6701 mL 1.3402 mL 3.3506 mL
40 mM 0.1005 mL 0.5026 mL 1.0052 mL 2.5130 mL
50 mM 0.0804 mL 0.4021 mL 0.8041 mL 2.0104 mL
60 mM 0.0670 mL 0.3351 mL 0.6701 mL 1.6753 mL
80 mM 0.0503 mL 0.2513 mL 0.5026 mL 1.2565 mL
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Pyrimethamine Related Classifications

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:

Pyrimethamine58-14-0Pirimecidan Pirimetamin RP 4753RP4753RP 4753RP-4753AntifolateParasiteantimalarialnucleoprotein metabolismfolic–folinic acid systemsparasitescell divisionInhibitorinhibitorinhibit

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