2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Anti-infection
  3. Antifolate Drug Metabolite Dihydrofolate reductase (DHFR) Parasite
  4. Methotrexate metabolite

Methotrexate metabolite  (Synonyms: DAMPA)

Cat. No.: HY-108251 Purity: 98.44%
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Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC50 values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation.

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

Methotrexate metabolite Chemical Structure

Methotrexate metabolite Chemical Structure

CAS No. : 19741-14-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Methotrexate metabolite:

Methotrexate metabolite Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Methotrexate metabolite

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • Biological Activity

  • Purity & Documentation

  • References

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Description

Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC50 values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation[2][3].

In Vitro

Methotrexate metabolite (100 mM, 24 h) is not cytotoxic in the Molt-4 human leukemic cell line[3].

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

Methotrexate metabolite Related Antibodies

Cell Cytotoxicity Assay[3]

Cell Line: Molt-4 human leukemic cell line
Concentration: 100 mM
Incubation Time: 48 h
Result: Alone was not cytotoxic to Molt-4 human leukemia cells at concentrations up to 100 mM, and DAMPA did not significantly alter the cytotoxicity profile of Methotrexate (HY-14519).
In Vivo

Methotrexate metabolite (8.6-10.1 mg/kg, 200 mg/m2, i.v., 15 minutes) has pharmacokinetic properties of rapid clearance and extensive metabolism in adult male Rhesus monkeys (Macaca mulatta) (8.0-15.9 kg), with an average clearance rate of 1.9 l/kg/h and an average terminal half-life of 51 minutes[1].

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

325.33

Formula

C15H15N7O2
CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

O=C(O)C1=CC=C(N(CC2=NC3=C(N)N=C(N)N=C3N=C2)C)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (15.37 mM; ultrasonic and warming and heat to 60°C; 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 3.0738 mL 15.3690 mL 30.7380 mL
5 mM 0.6148 mL 3.0738 mL 6.1476 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 (7.68 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.68 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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: 98.44%

COA (245 KB) RP-HPLC (252 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, 6 months; -20°C, 1 month. 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 3.0738 mL 15.3690 mL 30.7380 mL 76.8451 mL
5 mM 0.6148 mL 3.0738 mL 6.1476 mL 15.3690 mL
10 mM 0.3074 mL 1.5369 mL 3.0738 mL 7.6845 mL
15 mM 0.2049 mL 1.0246 mL 2.0492 mL 5.1230 mL
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Methotrexate metabolite 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:

Methotrexate metabolite19741-14-1DAMPAAntifolateDrug MetaboliteDihydrofolate reductase (DHFR)Parasitedihydrofolate reductasefolateInhibitorinhibitorinhibit

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