Diminazene Aceturate

Catalog No.S4104 Batch:S410401

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Technical Data

Formula

C14H15N7.2C4H7NO3

Molecular Weight 515.52 CAS No. 908-54-3
Solubility (25°C)* In vitro Water 103 mg/mL (199.79 mM)
DMSO 19 mg/mL (36.85 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
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)

Selleck's Diminazene Aceturate has been cited by 4 publications

Identification and targeting of microbial putrescine acetylation in bloodstream infections [ bioRxiv, 2023, 2023.09.21.558834] PubMed: 37790300
Identification and targeting of microbial putrescine acetylation in bloodstream infections [ bioRxiv, 2023, 10.1101/2023.09.21.558834] PubMed: 37790300
Lactate Dehydrogenase as a Potential Therapeutic Drug Target to Control Babesia bigemina [ Front Cell Infect Microbiol, 2022, 12:870852] PubMed: 35521220
Acid exposure disrupts mucus secretion and impairs mucociliary transport in neonatal piglet airways. [ Am J Physiol Lung Cell Mol Physiol, 2020, 10.1152/ajplung.00025.2020] PubMed: 32160007

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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