| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| ln Vitro |
Diminazene aceturate did not alter different TLRs on macrophages and dendritic cells, including TLR2, TLR4, and TLR9, when assessed by flow cytometry, suggesting that it may actually have a negative effect on the production of pro-inflammatory cytokines induced by LPS, CpG, and Poly I:C. Diminazene aceturate, on the other hand, dramatically reduced the phosphorylation of the NFκB p65 subunit, STAT (STAT1 and STAT3), and MAPK (ERK, p38, and JNK), which are important signaling molecules and pro-factors involved in the synthesis of pro-inflammatory cytokines [2].
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| ln Vivo |
Diminazene aceturate (14 mg/kg; intraperitoneal; female BALB/c and C57BL/6 mice) dramatically decreased both the total number of regulatory (CD4+Foxp3+) T cells and the total number of CD25+ cells. Disease-promoter-inflammatory cytokine levels in serum, including TNF, IFN-γ, IL-6, and IL-12 [1].
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| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse and C57BL/6 mice (6-8 weeks old) were infected with Trypanosoma congolense variant antigen type TC1[1]
Doses: 14 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: CD25+ cells The percentage of regulatory (CD4+Foxp3+) T cells was Dramatically diminished, and the serum levels of disease-reducing, exacerbating pro-inflammatory cytokines including IL-6, IL-12, TNF, and IFN were Dramatically diminished. -γ. |
| 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.
[2]. Kuriakose S, et al. Diminazene aceturate (Berenil), a new use for an old compound? Int Immunopharmacol. 2014 Aug;21(2):342-5. [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. |
| Additional Infomation |
Diminazene diaceturate is an N-acetylglycinate salt resulting from the reaction of diminazene with 2 mol eq. of N-acetylglycine. It has a role as an antiparasitic agent and a trypanocidal drug. It contains a diminazene(2+).
See also: Diminazene (annotation moved to). |
| Molecular Formula |
C14H15N7.2C4H7NO3
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|---|---|
| Molecular Weight |
515.52
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| Exact Mass |
515.224
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| CAS # |
908-54-3
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| Related CAS # |
536-71-0;908-54-3 (diaceturate);15114-96-2 (monoaceturate);31384-83-5 (2HCl);
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| PubChem CID |
5284544
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
463.3ºC at 760mmHg
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| Flash Point |
234ºC
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| LogP |
3.234
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
37
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| Complexity |
500
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CNC(C)=O)O.N=C(C1C=CC(N=NNC2C=CC(C(N)=N)=CC=2)=CC=1)N
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| InChi Key |
OKQSSSVVBOUMNZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H15N7.2C4H7NO3/c15-13(16)9-1-5-11(6-2-9)19-21-20-12-7-3-10(4-8-12)14(17)18;2*1-3(6)5-2-4(7)8/h1-8H,(H3,15,16)(H3,17,18)(H,19,20);2*2H2,1H3,(H,5,6)(H,7,8)
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| Chemical Name |
2-acetamidoacetic acid;4-[2-(4-carbamimidoylphenyl)iminohydrazinyl]benzenecarboximidamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~96.99 mM)
DMSO : ~25 mg/mL (~48.49 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1940 mL | 0.9699 mL | 1.9398 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03755752 | COMPLETED | Procedure: Phacoemulsification with and without Trypan Blue capsule staining |
Cataract Diabetic | Assiut University | 2018-01-01 | Not Applicable |
| NCT01621789 | COMPLETED | Other: dye of lutein, zeaxanthin, trypan blue | Cataract | Federal University of São Paulo | 2012-06 | Phase 3 |
| NCT00757380 | COMPLETED | Procedure: Trypan Blue Procedure: Brillant Blue |
Idiopathic Epiretinal Membranes | The Ludwig Boltzmann Institute of Retinology and Biomicroscopic Laser Surgery |
2008-07 | Not Applicable |
| NCT00419185 | COMPLETED | Procedure: Delamination of the Internal limiting membrane | Idiopathic Macular Hole | University of Luebeck | 2003-04 | Not Applicable |
| NCT01385878 | UNKNOWN STATUS | Procedure: Microcoaxial Phacoemulsification Procedure: Microcoaxial Phacoemulsification |
Cataract | Iladevi Cataract and IOL Research Center | 2011-01 | Not Applicable |
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