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Diminazene Aceturate Parasite inhibitor

Name: Diminazene Aceturate
Brand: Selleck Chemicals
SKU: S4104
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S4104

Diminazene(Diminazene diaceturate) is a di-amidine also known as 4,4-(1-Triazene–1,3–diyl)bis(benzenecarboximidamide), used as an effective trypanocidal agent. 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.

Chemical Structure

Molecular Weight: 515.52

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Quality Control

Batch: S410401 Water]103 mg/mL]false]DMSO]19 mg/mL]false]Ethanol]Insoluble]false Purity: 99.09%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.09

Related Targets	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Reverse Transcriptase HIV HCV Protease
Other Parasite Inhibitors	Oxibendazole Avermectin B1 (+/-)-nerolidol Milbemycin Oxime Arteether Eprinomectin Emodepside Diclazuril Selamectin Oxfendazole

Solubility

In vitro
Batch:

Water : 103 mg/mL

DMSO : 19 mg/mL (36.85 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.05mg/ml (0.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 1 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	515.52	Formula	C₁₄H₁₅N₇.2C₄H₇NO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	908-54-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Diminazene diaceturate			Smiles	CC(=O)NCC(=O)O.CC(=O)NCC(=O)O.C1=CC(=CC=C1C(=N)N)NN=NC2=CC=C(C=C2)C(=N)N

Mechanism of Action

In vitro	Diminazene is capable of inhibiting the P2 transporter activity and this activity is lost in one diminazene-adapted trypanosome line, this does not formally prove that TbAT1 transports diminazene, nor does it establish whether transporter in addition to P2 could be involved in diminazene uptake. Diminazene is rapidly accumulated through a single transporter in T. brucei brucei 427 with K_m value of 0.45 μM. [³H]Diminazene transport is also potently inhibited by pentamidine and adenosine, with K_i values of 0.21 μM and 0.25 μM, respectively. [3H]diminazene (2.5 μM) is clearly accumulated by yeast cells expressing TbAT1, with a rate of 0.0083 pmol/10⁷ cell/s, and this process is completely inhibited by the presence of 1 mM unlabeled diminazene aceturate.
In vivo	Diminazene aceturate (3.5 mg/kg) appeares to be effective in the first treatment of horses and mules infected with T. evansi, parasites are cleared from the peripheral blood of horses on days 1 and 7 and mules on days 1 and 14. Diminazene aceturate (DA) (7 mg/kg, i.m.) effectively clears the parasites from the blood of the infected treated dogs.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15105099/ [2] https://pubmed.ncbi.nlm.nih.gov/12482651/ [3] https://pubmed.ncbi.nlm.nih.gov/18155842/

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