2. Cell Cycle/DNA Damage Anti-infection
  3. Antifolate Bacterial
  4. Diaveridine

Diaveridine  (Synonyms: EGIS-5645)

Cat. No.: HY-B1902 Purity: 99.79%
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Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.

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

Diaveridine Chemical Structure

Diaveridine Chemical Structure

CAS No. : 5355-16-8

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Diaveridine:

Diaveridine Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.

IC50 & Target

Ki: 11.5 nM (DHFR) [1]
Bacterial[2]
Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 1000 μM
Compound: Diaveridine
Cytotoxicity against human A549 cells after 24 to 48 hrs by fluorescence-based assay
Cytotoxicity against human A549 cells after 24 to 48 hrs by fluorescence-based assay
[PMID: 29784273]
In Vitro

Diaveridine is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent[1]. Treatments with Diaveridine for 90 min have a strong bactericidal effect on S. typhimurium TA1535, and no bacterial growth is observed at 10μg/mL or more. Without metabolic activation, treatment with Diaveridine for 48 h, but not 24 h, causes a dose-dependent, significant increase in the frequency of aberrant metaphases. At 100 μg/mL, 60% of the metaphases contain chromosome aberrations[2].

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

Diaveridine Related Antibodies
In Vivo

The sperm abnormality of the Diaveridine (DVD) treatment groups at all dose levels (Diaveridine, 128 to 512 mg/kg) shows no significant differences compare with the negative control group. There are no significant differences of micronucleus between the negative control group and the Diaveridine treatment groups (Diaveridine, 128 to 512 mg/kg). The chromosome aberration of the Diaveridine treatment groups at all dose levels and the negative control group are significantly lower than those in the positive control group treated with cyclophosphamide (P<0.05), indicating that Diaveridine at the doses studied does not cause abnormal chromosome aberration. The results demonstrate that the Diaveridine administration does not produce significant changes in the ratio of organ-to-body weight, compare with the negative control group in the end period of the study[3].

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

260.29

Formula

C13H16N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC=C(CC2=CC=C(OC)C(OC)=C2)C(N)=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 : 33.33 mg/mL (128.05 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 3.8419 mL 19.2093 mL 38.4187 mL
5 mM 0.7684 mL 3.8419 mL 7.6837 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.

  • Molarity Calculator

  • 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 (9.60 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 (9.60 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
References
Cell Assay
[2]

Cells are cultured at 37°C in a humidified atmosphere of 5% CO2 in air. The growth medium is Eagle’s MEM supplemented with 10% fetal bovine serum. In the experiment without metabolic activation, the cells are treated for 24 or 48 h continuously without a medium change. In the experiment with metabolic activation, the cells are pulse treated with test compounds (including Diaveridine) at varying doses for 6 h and incubated for 18 h in fresh culture medium. Breakage type chromatid aberrations, exchange type chromatid aberrations, breakage type chromosome aberrations, and exchange type chromosome aberrations are scored. Gaps are also counted. Mitotic index is determined from scoring 2000 cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration

3]Fifty male ICR mice, weighing 25 to 35 g, are assigned to five groups randomly with 10 mice in each group. Mice in the experiment groups receive Diaveridine (DVD) via IG at ed 128 mg/kg (low doses), 256 mg/kg (medium doses), and 512 mg/kg (high doses) body weight for 5 consecutive days, respectively. Mice in negative and positive control groups receive IG 1% CMC-Na solvent and 40 mg/kg body weight of cyclophosphamide, respectively. The testing groups are administered 0.2 mL/10 g Diaveridine (mixed with 1% of CMC-Na, to obtain the concentration of 2 mg/mL.) body weight, once a day, for 5 days. The behavioral changes are recorded on the daily basis[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 3.8419 mL 19.2093 mL 38.4187 mL 96.0467 mL
5 mM 0.7684 mL 3.8419 mL 7.6837 mL 19.2093 mL
10 mM 0.3842 mL 1.9209 mL 3.8419 mL 9.6047 mL
15 mM 0.2561 mL 1.2806 mL 2.5612 mL 6.4031 mL
20 mM 0.1921 mL 0.9605 mL 1.9209 mL 4.8023 mL
25 mM 0.1537 mL 0.7684 mL 1.5367 mL 3.8419 mL
30 mM 0.1281 mL 0.6403 mL 1.2806 mL 3.2016 mL
40 mM 0.0960 mL 0.4802 mL 0.9605 mL 2.4012 mL
50 mM 0.0768 mL 0.3842 mL 0.7684 mL 1.9209 mL
60 mM 0.0640 mL 0.3202 mL 0.6403 mL 1.6008 mL
80 mM 0.0480 mL 0.2401 mL 0.4802 mL 1.2006 mL
100 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.9605 mL
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Diaveridine 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:

Diaveridine5355-16-8EGIS-5645EGIS5645EGIS 5645AntifolateBacterialInhibitorinhibitorinhibit

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