Diminazene Aceturate

Catalog No.S4104

For research use only.

Diminazene 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

Selleck's Diminazene Aceturate has been cited by 2 Publications

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Biological Activity

Description Diminazene 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.
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 Km value of 0.45 μM. [3H]Diminazene transport is also potently inhibited by pentamidine and adenosine, with Ki 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 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]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 515.52
Formula

C14H15N7.2C4H7NO3

CAS No. 908-54-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

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