Diminazene aceturate
Based on 11 publication(s) in Google Scholar
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.
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- Purity: 99.39%
- CAS No.: 908-54-3
- 화학식: C22H29N9O6
- 분자량:515.52
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Diminazene aceturate
More- Cell Metab. 2022 Mar 1;34(3):424-440.e7. [Abstract]
- Int J Radiat Oncol Biol Phys. 2025 Sep 16:S0360-3016(25)06272-8. [Abstract]
- Drug Deliv Transl Res. 2025 Oct 29. [Abstract]
- Int Immunopharmacol. 2025 Aug 11:164:115325. [Abstract]
- Neuropharmacology. 2026 May 15:289:110880. [Abstract]
- FASEB J. 2026 Mar 31;40(6):e71682. [Abstract]
- J Inflamm Res. 2023 Apr 17:16:1639-1652. [Abstract]
- Endocrine. 2021 May;72(2):340-348. [Abstract]
- Radiat Res. 2022 Oct 1;198(4):325-335. [Abstract]
- Parasitol Res. 2025 Dec 3;124(12):149. [Abstract]
- Research Square Preprint. 2021 Mar.
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IHC
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In Vivo Efficacy Study
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IHC
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Bio/Physico-chemical Assay
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Biological Activity
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Trypanosoma |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | CC50 |
38.5 μM
Compound: Diminazene aceturate
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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
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[PMID: 33479668] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice and C57BL/6 mice (6-8 week old) infected with T. congolense variant antigenic type TC1[1]
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Dosage:14 mg/kg
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Administration:Intraperitoneal injection
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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.
Chemical Information
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CAS No. 908-54-3
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Appearance Solid
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분자량 515.52
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화학식 C22H29N9O6
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Color Light yellow to yellow
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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
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Synonyms
Diminazene diaceturate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (11)
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Journal Impact Factor
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Most Recent
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Cell Metab
Imatinib and methazolamide ameliorate COVID-19-induced metabolic complications via elevating ACE2 enzymatic activity and inhibiting viral entry. [Abstract]2022 Mar 1;34(3):424-440.e7. PMID: 35150639
Diminazene aceturate purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Mar 1;34(3):424-440.e7. [Abstract]
The direct binding was illustrated by surface plasmon resonance (SPR) assay of purified ACE2 protein with Diminazene aceturate (DIZE;0.125, 0.25, 0.5, 1, 2 μM).
Diminazene aceturate purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Mar 1;34(3):424-440.e7. [Abstract]
HUVECs were treated with Diminazene aceturate (DIZE, 100 μM), imatinib (Ima), harpagoside (Har) or methazolamide (Met) for 16 h and subjected to real-time PCR
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Int J Radiat Oncol Biol Phys
Activation of Angiotensin Converting Enzyme 2 (ACE2) Mitigates Gastrointestinal Acute Radiation Syndrome (GI-ARS). [Abstract]2025 Sep 16:S0360-3016(25)06272-8. PMID: 40967372
Diminazene aceturate purchased from MedChemExpress. Usage Cited in: Int J Radiat Oncol Biol Phys. 2025 Sep 16:S0360-3016(25)06272-8. [Abstract]
Diminazene aceturate (DIZE; 15 mg/kg; SC）showed a near depletion of Ki-67+ regenerating intestinal crypts. WAG/RijCmcr rats were exposed to 12.5 Gy PBI and treated subcutaneously with vehicle or Diminazene aceturate (DIZE; 15 mg/kg; SC on days 3, 4, and 5 postirradiation. Representative Ki-67-stained IHC cross-sections of day 6 jejunum from nonirradiated, 12.5 Gy + vehicle-treated, or 12.5 Gy + DIZE.
Diminazene aceturate purchased from MedChemExpress. Usage Cited in: Int J Radiat Oncol Biol Phys. 2025 Sep 16:S0360-3016(25)06272-8. [Abstract]
Diminazene aceturate (DIZE; 15 mg/kg; SC）showed a decrease in plasma citrulline levels indicative of reduced GI mass in WAG/RijCmcr rats. Mean plasma citrulline levels at day 6 in female and male rats after irradiation and treatment with vehicle or DIZE.
Diminazene aceturate purchased from MedChemExpress. Usage Cited in: Int J Radiat Oncol Biol Phys. 2025 Sep 16:S0360-3016(25)06272-8. [Abstract]
Diminazene aceturate (DIZE; 15 mg/kg; SC) increased luminal ACE2 staining. Representative ACE2-stained IHC cross-sections of day 6 jejunums from nonirradiated, 12.5 Gy + vehicle-treated, or 12.5 Gy + DIZE.
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Drug Deliv Transl Res
Leveraging quantum chemical properties in transfer learning for predicting blood-brain barrier permeability of drugs. [Abstract]2025 Oct 29. PMID: 41160380 -
Int Immunopharmacol
ACE2/Ang(1-7)/MasR axis exerts protective effects on lung ischemia/reperfusion injury via NF-κB-dependent mitochondrial adaptation and epithelial cell pyroptosis. [Abstract]2025 Aug 11:164:115325. PMID: 40795499 -
Neuropharmacology
Diminazene attenuates astrocytic oxidative stress and neuronal ferroptosis via miR-10b-3p/NOX4 axis in Alzheimer's Disease Model. [Abstract]2026 May 15:289:110880. PMID: 41698644 -
FASEB J
Diminazene Aceturate Ameliorates Hypertension-Induced Cognitive Impairment by Disrupting the CCN1-Integrin αvβ6-TGF-β Axis and Preserving Mitochondrial Integrity. [Abstract]2026 Mar 31;40(6):e71682. PMID: 41860098 -
J Inflamm Res
Diminazene Ameliorates Neuroinflammation by Suppression of Astrocytic miRNA-224-5p/NLRP3 Axis in Alzheimer's Disease Model. [Abstract]2023 Apr 17:16:1639-1652. PMID: 37092127 -
Endocrine
A potential impact of SARS-CoV-2 on pituitary glands and pituitary neuroendocrine tumors. [Abstract]2021 May;72(2):340-348. PMID: 33786714 -
Radiat Res
2022 Oct 1;198(4):325-335. PMID: 35904437 -
Parasitol Res
Furamidine, a methyltransferase inhibitor, is a potential anti-Babesia spp. chemotherapeutic. [Abstract]2025 Dec 3;124(12):149. PMID: 41339613 -
용액&용해도
H2O : 50 mg/mL (96.99 mM; Need ultrasonic)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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Data Sheet (277 KB)
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References
[1]. Kuriakose S, et al. Diminazene aceturate (Berenil) modulates the host cellular and inflammatory responses to Trypanosoma congolense infection. PLoS One. 2012;7(11):e48696. [Content Brief]
[2]. Kuriakose S, et al. Diminazene aceturate (Berenil), a new use for an old compound? Int Immunopharmacol. 2014 Aug;21(2):342-5. [Content Brief]
[3]. Castardeli C, et al. The ACE 2 activator diminazene aceturate (DIZE) improves left ventricular diastolic dysfunction following myocardial infarction in rats. Biomed Pharmacother. 2018 Nov;107:212-218. [Content Brief]
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 |
|---|---|---|---|---|---|
| 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 | |
| 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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