Structure of Diminazene aceturate
CAS No.: 908-54-3
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Diminazene Aceturate is a di-amidine used as an effective trypanocidal agent.
Synonyms: Diminazene diaceturate; Diminazene (aceturate)
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CAS No. : | 908-54-3 |
Formula : | C22H29N9O6 |
M.W : | 515.52 |
SMILES Code : | N=C(N)C1=CC=C(/N=N/NC2=CC=C(C=C2)C(N)=N)C=C1.O=C(O)CNC(C)=O.O=C(O)CNC(C)=O |
Synonyms : |
Diminazene diaceturate; Diminazene (aceturate)
|
MDL No. : | MFCD00058386 |
InChI Key : | OKQSSSVVBOUMNZ-UHFFFAOYSA-N |
Pubchem ID : | 5284544 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
Trypanosoma equiperdum | 5 μM | 60 minutes | Promotes linearization of mitochondrial minicircle DNA, forming DNA-protein complexes | PMC53387 |
NRCMs | 100 nM | 48 hours | To evaluate the protective effect of DIZE on PM2.5-induced cardiomyocyte apoptosis. Results showed that DIZE pretreatment upregulated ACE2 expression and suppressed Bax/Bcl-2 and cleaved caspase3/total caspase3 ratios, alleviating PM2.5-induced cardiomyocyte apoptosis. | PMC9089227 |
Human CD34+ cells | 100 nM | 10 hours | To evaluate the effect of DIZE on the migratory capacity of CD34+ cells from PH patients, results showed significant improvement in migration | PMC3733435 |
Recombinant human ACE2 | 100 μM | To evaluate the effect of DIZE on ACE2 enzymatic activity, results showed a twofold increase in ACE2 activity | PMC3733435 | |
Primary cultured human retinal pigment epithelia (hRPE) | 10 μg/mL | 6 hours | DIZE significantly increased the expression of ACE2 and inhibited the expression of IL-6, IL-8, and MCP-1 at both mRNA and protein levels in LPS-stimulated RPE cell lines. | PMC4748536 |
ARPE-19 cells | 10 μg/mL | 6 hours | DIZE significantly increased the expression of ACE2 and inhibited the expression of IL-6, IL-8, and MCP-1 at both mRNA and protein levels in LPS-stimulated RPE cell lines. | PMC4748536 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Mice | PM2.5-induced cardiac dysfunction model | Intraperitoneal injection | 15 mg/kg/day | Once daily for 30 days | To evaluate the therapeutic effect of DIZE on PM2.5-induced cardiac dysfunction. Results showed that DIZE treatment significantly reversed PM2.5-induced reduction in ejection fraction and fractional shortening, reduced cardiomyocyte apoptosis, upregulated cardiac ACE2 expression, and decreased Bax/Bcl-2 and cleaved caspase3/total caspase3 ratios. | PMC9089227 |
Mice | Tg2576 mouse model | Intraperitoneal injection | 15 mg/kg/day | Daily for 30 days or 10 weeks | DIZE, by enhancing ACE2 activity, reduced hippocampal Aβ pathology and restored cognitive function. In symptomatic aged Tg2576 mice, DIZE restored cognitive function; in pre-symptomatic young mice, DIZE prevented the onset of cognitive impairment. | PMC7035243 |
C57BL/6 mice | Repeated LPS-induced neuroinflammation model | Intraperitoneal injection | 15 mg/kg | Daily administration for 2 weeks | To evaluate the neuroprotective effects of DIZE via activation of ACE2/Ang(1–7)/MasR axis in neuroinflammation. Results demonstrated that DIZE treatment significantly attenuated LPS-induced overactivation of ACE/AngII/AT1 axis, restored the balance of ACE2/Ang(1–7)/MasR axis, and suppressed microglial proinflammatory polarization through FOXO1-autophagy pathway. | PMC8520723 |
Rats | Myocardial infarction model | Subcutaneous injection | 15 mg/kg/day | Once daily, continued throughout the study period | DIZE treatment attenuated the MI-induced decrease in cardiac function, improved hemodynamic function, reduced ventricular hypertrophy, and restored the normal balance of the cardiac renin-angiotensin system. | PMC3881360 |
Ldlr−/− mice | AngII-induced abdominal aortic aneurysms | Intramuscular injection | 30 mg/kg/day | Daily for 28 days | DIZE significantly decreased aortic lumen diameters and aortic external diameters of AngII-infused mice resulting in a marked reduction in AAA incidence (from 73 to 29%). None of these effects of DIZE were observed in the Ace2?/y mice. | PMC4250973 |
Sprague Dawley rats | Endothelin-1-induced ischemic stroke model | Intraperitoneal injection | 0.75, 2.5, 7.5, 15 mg/kg | Administered at 4h, 1d, and 2d post-stroke | To evaluate the neuroprotective effects of Diminazene aceturate post-stroke. Results showed that 7.5 mg/kg dose significantly reduced infarct volume and improved neurological function. | PMC4465873 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT01477749 | Cancer of Prostate ... More >> Cancer of the Prostate Neoplasms, Prostate Neoplasms, Prostatic Prostate Cancer Prostate Neoplasms Prostatic Cancer Less << | Phase 2 | Completed | - | Austria ... More >> Ludwig Boltzmann-Institute for Applied Cancer Research Wien, Austria, A-1100 France Department of Cancer Medicine and Genitourinary Oncology Group Institut Gustave Roussy (IGR) Département de médicine Vaillant, Villejuif Cedex, France, 94805 Netherlands Radboud University Nijmegen; UMC St Radboud Hospital; Faculteit der Medische Wetenschappen, Urologie Nijmegen, Gelderland, Netherlands, 6525 GA United Kingdom Barts Cancer Institute - a Cancer Research UK Centre of Excellence, Queen Mary University of London London, United Kingdom, EC1M 6BQ Less << |
NCT02983344 | Femoral Fracture | Not Applicable | Completed | - | Malaysia ... More >> Kuala Lumpur General Hospital Kuala Lumpur, Wilayah Persekutuan, Malaysia, 50586 Less << |
NCT01250509 | Obesity | Phase 2 | Completed | - | United States, California ... More >> UCSF Osher Center for Integrative Medicine San Francisco, California, United States, 94115 Less << |
NCT01477749 | - | Completed | - | - | |
NCT02373137 | Keratoplasty ... More >>Grafting, Corneal Transplantation, Corneal Transplantation, Cornea Keratoplasty, Lamellar Less << | Phase 4 | Active, not recruiting | December 2019 | United States, California ... More >> Byers Eye Institute, Stanford University Palo Alto, California, United States, 94303 F. I. Proctor Foundation, University of California, San Francisco San Francisco, California, United States, 94143 United States, Oregon Casey Eye Institute, Oregon Health & Science University Portland, Oregon, United States, 97239 Less << |
NCT02235051 | Cancer Survivor ... More >> Estrogen Receptor-positive Breast Cancer Stage IA Breast Cancer Stage IB Breast Cancer Stage IIA Breast Cancer Stage IIB Breast Cancer Stage IIIA Breast Cancer Postmenopausal Less << | Not Applicable | Active, not recruiting | September 2019 | United States, California ... More >> City of Hope Medical Center Duarte, California, United States, 91010 Less << |
NCT01250509 | - | Completed | - | - | |
NCT01674439 | Craniofacial Microsomia | Phase 2 | Completed | - | Brazil ... More >> Division of Plastic and Reconstructive Surgery Sao Paulo, SP, Brazil, 01246000 Less << |
NCT01218750 | Diffuse Diabetic Macular Edema | Not Applicable | Unknown | December 2011 | Poland ... More >> Military Institute of Medicine Recruiting Warsaw, Szaserów 44, Poland, 04-141 Contact: Kowal Ewelina (+48) 22 665 707 584 ekowal@wim.mil.pl Principal Investigator: Robaszkiewicz Jacek, dr med. Sub-Investigator: Chmielewska I. Katarzyna, lek. med. Less << |
NCT02073266 | Macular Holes ... More >> Visual Acuity Gain Cataract Complications Less << | Not Applicable | Completed | - | Canada, Quebec ... More >> Centre universitaire d'ophtalmologie, Hôpital du Saint-Sacrement, CHU de Québec Québec, Quebec, Canada, G1S 4L8 Less << |
NCT01228188 | Macular Holes | Not Applicable | Unknown | August 2013 | Poland ... More >> Military Institute of Medcine Recruiting Warsaw, ul. Szaserów 128, Poland, 04-141 Contact: Połeć Dorota, mgr + 48 22 681 67 35 dpolec@wim.mil.pl Principal Investigator: Robaszkiewicz Jacek, dr med. Sub-Investigator: Chmielewska I. Katarzyna, lek. med. Sub-Investigator: Karpińska Urszula, lek. med. Less << |
NCT00302328 | Idiopathic Macular Hole | Not Applicable | Completed | - | Denmark ... More >> Department of Ophthalmology, Glostrup Hospital Copenhagen, Denmark, DK-2600 Less << |
NCT02126280 | - | Completed | - | Russian Federation ... More >> Institute for Atherosclerosis Research Moscow, Russian Federation, 121609 Less << | |
NCT01485575 | - | Recruiting | June 2020 | Austria ... More >> General Hospital Linz Recruiting Linz, Austria, 4010 Contact: Rupert W Strauss, MD +43 732 7806 - 73425 rupert.strauss@akh.linz.at Switzerland St. Gallen Hospital Recruiting St. Gallen, SG, Switzerland, 9007 Contact: Christophe Valmaggia, MD +41 71 494 11 11 Christophe.Valmaggia@kssg.ch Kantonsspital Winterthur, Eye Clinic Recruiting Winterthur, Switzerland, 8401 Contact: Paul B Henrich, MD +41 52 266 28 95 bernhard.henrich@ksw.ch Less << | |
NCT01385878 | Cataract | Not Applicable | Unknown | December 2011 | India ... More >> Iladevi Cataract & IOL Research Centre Recruiting Ahmedabad, Gujarat, India, 380009 Contact: Abhay r Vasavada, MS,FRCS icirc@abhayvasavada.com Principal Investigator: Abhay R Vasavada, MS, FRCS Less << |
NCT02466256 | Cataract | Not Applicable | Completed | - | - |
NCT03755752 | Cataract Diabetic | Not Applicable | Completed | - | Egypt ... More >> Faculty of Medicine Assiut, Egypt, 71515 Less << |
NCT01621789 | Cataract | Phase 3 | Completed | - | Brazil ... More >> Dept. of Ophthalmology - UNIFESP/Hospital São Paulo São Paulo, SP, Brazil, 04023-062 Less << |
NCT00302328 | - | Completed | - | - | |
NCT00757380 | Idiopathic Epiretinal Membrane... More >>s Less << | Not Applicable | Completed | - | Austria ... More >> The Ludwig Boltzmann Institute of Retinology and Biomicroscopic Laser Surgery Vienna, Austria, 1030 Less << |
NCT00419185 | Idiopathic Macular Hole | Not Applicable | Completed | - | Germany ... More >> Eye Clinic, University Schleswig-Holstein, Campus Lübeck Lübeck, Schleswig-Holstein, Germany, 23538 Less << |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.94mL 0.39mL 0.19mL |
9.70mL 1.94mL 0.97mL |
19.40mL 3.88mL 1.94mL |
Tags: Diminazene | Diminazene diaceturate | Parasite | Angiotensin-converting Enzyme | Diminazene aceturate | anti-trypanosomal agent | kinetoplast DNA | ACE2 activator | anti-inflammatory | trypanocidal action | angiotensin-converting enzyme 2 | 908-54-3
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H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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