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Diminazene Aceturate

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

Synonyms: Diminazene diaceturate

Catalog No.S4104 Purity:99.09%

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.

Diminazene Aceturate Chemical Structure

CAS No. 908-54-3

Purity & Quality Control

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

99.09

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Biological Activity

Description

In vitro
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. ^[1]

In Vivo
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. ^[2] Diminazene aceturate (DA) (7 mg/kg, i.m.) effectively clears the parasites from the blood of the infected treated dogs. ^[3]

References

Chemical Information & Solubility

Molecular Weight	515.52	Formula	C₁₄H₁₅N₇.2C₄H₇NO₃
CAS No.	908-54-3	SDF	Download Diminazene Aceturate SDF
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
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

Water : 103 mg/mL

DMSO : 19 mg/mL ( (36.85 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

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 Dosing volume per animal:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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