2. Anti-infection Metabolic Enzyme/Protease
  3. Parasite Angiotensin-converting Enzyme (ACE)
  4. Diminazene aceturate

Diminazene aceturate  (Synonyms: Diminazene diaceturate)

Cat. No.: HY-12404 Purity: 99.16%
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Diminazene aceturate (Diminazene diaceturate) is an anti-trypanosome agent for livestock. The main biochemical mechanism of the trypanocidal actions of Diminazene aceturate is by binding to trypanosomal kinetoplast DNA (kDNA) in a non-intercalative manner through specific interaction with sites rich in adenine-thymine base pairs. Diminazene aceturate is also an angiotensin-converting enzyme 2 (ACE2) activator and has strong and potent anti-inflammatory properties.

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

Diminazene aceturate Chemical Structure

Diminazene aceturate Chemical Structure

CAS No. : 908-54-3

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Based on 5 publication(s) in Google Scholar

Other Forms of Diminazene aceturate:

Diminazene aceturate Related Antibodies

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

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  • References

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Description

Diminazene aceturate (Diminazene diaceturate) is an anti-trypanosome agent for livestock. The main biochemical mechanism of the trypanocidal actions of Diminazene aceturate is by binding to trypanosomal kinetoplast DNA (kDNA) in a non-intercalative manner through specific interaction with sites rich in adenine-thymine base pairs. Diminazene aceturate is also an angiotensin-converting enzyme 2 (ACE2) activator and has strong and potent anti-inflammatory properties[1][2][3].

IC50 & Target

Trypanosoma

 

Cellular Effect
Cell Line Type Value Description References
HEK293 CC50
38.5 μM
Compound: Diminazene aceturate
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability measured after 48 hrs by resazurin assay
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability measured after 48 hrs by resazurin assay
[PMID: 33479668]
In Vitro

Pre-treatment of bone marrow-derived macrophages (BMDM) and dendritic cells (BMDC) with Diminazene aceturate (Berenil) downregulats LPS-, CpG- and Poly I:C-induced proinflammatory cytokine production, suggesting that it may be affecting common pathways through which these molecules stimulate proinflammatory cytokine production. Indeed, Diminazene aceturate does not alter the expression of different TLRs (including TLR2, TLR4 and TLR9), on macrophages and DCs when assessed by flow cytometry. Instead, Diminazene aceturate dramatically downregulats the phosphorylation of MAPKs (ERK, p38 and JNK), STATs (STAT1 and STAT3) and NFκB p65 subunit, which are key signaling molecules and transcription factors involved in the production of proinflammatory cytokines[2].

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

Diminazene aceturate Related Antibodies
In Vivo

Diminazene aceturate (14 mg/kg; intraperitoneal injection; female BALB/c mice and C57BL/6 mice) treatment significantly reduces the percentages of CD25+ cells, a concomitant reduction in the percentage of regulatory (CD4+Foxp3+) T cells and a striking reduction in serum levels of disease exacerbating pro-inflammatory cytokines including IL-6, IL-12, TNF and IFN-γ[1].

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

Animal Model: Female BALB/c mice and C57BL/6 mice (6-8 week old) infected with T. congolense variant antigenic type TC1[1]
Dosage: 14 mg/kg
Administration: Intraperitoneal injection
Result: Significantly reduced the percentages of CD25+ cells, a concomitant reduction in the percentage of regulatory (CD4+Foxp3+) T cells and a striking reduction in serum levels of disease exacerbating pro-inflammatory cytokines including IL-6, IL-12, TNF and IFN-γ.
Molecular Weight

515.52

Formula

C22H29N9O6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O)CNC(C)=O.N=C(C1=CC=C(/N=N/NC2=CC=C(C(N)=N)C=C2)C=C1)N.O=C(O)CNC(C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (96.99 mM; Need ultrasonic)

DMSO : 25 mg/mL (48.49 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 1.9398 mL 9.6989 mL 19.3979 mL
5 mM 0.3880 mL 1.9398 mL 3.8796 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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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: ≥ 2.08 mg/mL (4.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.16%

SDS (394 KB)

COA (251 KB) HNMR (268 KB) LCMS (95 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 (sealed storage, away from moisture). 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 / H2O 1 mM 1.9398 mL 9.6989 mL 19.3979 mL 48.4947 mL
5 mM 0.3880 mL 1.9398 mL 3.8796 mL 9.6989 mL
10 mM 0.1940 mL 0.9699 mL 1.9398 mL 4.8495 mL
15 mM 0.1293 mL 0.6466 mL 1.2932 mL 3.2330 mL
20 mM 0.0970 mL 0.4849 mL 0.9699 mL 2.4247 mL
25 mM 0.0776 mL 0.3880 mL 0.7759 mL 1.9398 mL
30 mM 0.0647 mL 0.3233 mL 0.6466 mL 1.6165 mL
40 mM 0.0485 mL 0.2425 mL 0.4849 mL 1.2124 mL
H2O 50 mM 0.0388 mL 0.1940 mL 0.3880 mL 0.9699 mL
60 mM 0.0323 mL 0.1616 mL 0.3233 mL 0.8082 mL
80 mM 0.0242 mL 0.1212 mL 0.2425 mL 0.6062 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Diminazene aceturate 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:

Diminazene908-54-3Diminazene diaceturateParasiteAngiotensin-converting Enzyme (ACE)Inhibitorinhibitorinhibit

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