1. Anti-infection
  2. Parasite
  3. Acoziborole

Acoziborole (Synonyms: SCYX-7158; AN5568)

Cat. No.: HY-19910 Purity: 99.64%
Handling Instructions

Acoziborole (SCYX-7158) is an effective, safe and orally active antiprotozoal agent for the research of human african trypanosomiasis (HAT). In the T. b. brucei S427 strain, the MIC value for SCYX-7158 is 0.6 µg/mL.

For research use only. We do not sell to patients.

Acoziborole Chemical Structure

Acoziborole Chemical Structure

CAS No. : 1266084-51-8

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 385 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
250 mg USD 3800 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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Description

Acoziborole (SCYX-7158) is an effective, safe and orally active antiprotozoal agent for the research of human african trypanosomiasis (HAT). In the T. b. brucei S427 strain, the MIC value for SCYX-7158 is 0.6 µg/mL[1].

In Vitro

Acoziborole is active in vitro against relevant strains of Trypanosoma brucei, including T. b. rhodesiense and T. b. gambiense.In whole cell assays, Acoziborole exhibits potent activity against representative T. b. brucei, T. b. rhodesiense and T. b. gambiense strains. IC50 values for Acoziborole are approximately 0.07 µg/mL to 0.37 µg/mL following incubation of the parasite strains with Acoziborole for 72 h. In the T. b. brucei S427 strain, the MIC value for Acoziborole is 0.6 µg/mL, approximately two times the IC50 measured for this strain. In contrast to the potent activity of Acoziborole against trypanosomes, no significant inhibition of cell proliferation is observed in an in vitro mammalian cell (L929 mouse cell line) assay at drug concentrations up to 50 µg/mL. The potential for Acoziborole to inhibit cytochrome P450 (CYP) enzymes is evaluated using P450-Glo assays for the human isoforms CYP3A4, CYP1A2, CYP2C19, CYP2C9 and CYP2D6. The IC50 values for Acoziborole in these assays are all above 10 µM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In uninfected mice, 4.3 mg/kg intravenous dose of Acoziborole show an apparent elimination half-life (t1/2) of 26.6 h; systemic clearance (CL) of 0.089 L/h/kg; a volume of distribution (Vdss) of 1.69 L/kg and area under the concentration-time curve (AUC0-24 h) of 48 h•μg/mL. Following an oral dose of 13.4 mg/kg, which corresponds to the lowest efficacious dose in the murine stage 2 HAT model, Acoziborole is rapidly absorbed, as a Cmax of 6.96 µg/mL is achieved in plasma at 6 h after dose, with an oral clearance (Cl/F) value of 0.163 L/h/kg, an AUC0-24 h of 82 h•μg/mL and absolute oral bioavailability of 55%. After a 26 mg/kg oral dose, which corresponds to the dose giving a 100% cure rate in the murine stage 2 HAT model, Cmax increases to 9.8 µg/mL and the AUC0-24 h is 113 h•μg/mL. In uninfected rats, following oral administration of Acoziborole at a nominal dose of 25 mg/kg (dose affording a 100% cure rate in mice), Cmax increases approximately 2 fold more than that in mice (Cmax=18.2 µg/mL) and AUC0-24 h, and hence oral clearance, improves approximately 4 fold (AUC0-24 h 291 h•μg/mL and CL/F=0.092 L/kg/h). The time to maximum concentration is similar to that in mice (tmax=8 h). Uninfected male and female cynomolgus monkeys are treated with Acoziborole at 2 mg/kg (IV) on study day 1 and 10 mg/kg (NG) on study day 8. Acoziborole exhibits excellent plasma pharmacokinetics, with CL of 0.022 L/h/kg; Vdss of 0.656 L/kg and area under the concentration-time curve 78.8 h•μg/mL, and 94.4 for AUC0-24 h and AUC0-inf, respectively, following intravenous administration[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

367.10

Formula

C₁₇H₁₄BF₄NO₃

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (340.51 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7241 mL 13.6203 mL 27.2405 mL
5 mM 0.5448 mL 2.7241 mL 5.4481 mL
10 mM 0.2724 mL 1.3620 mL 2.7241 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 8 mg/mL (21.79 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 8 mg/mL (21.79 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Compounds (e.g., Acoziborole) to be tested are serially diluted in DMSO and added to 96-well plates to give final concentrations ranging from 5 to 0.01 µg/mL. T. b. brucei parasites in the log phase of growth are diluted in HMI-9 media and added to each well for a final concentration of 1×104 parasites per well. For the sensitivity assays using T. b. rhodesiense and T. b. gambiense, pararasites are cultured in MEM supplemented with Baltz components, diluted in the aforementioned culture media, and added to each well at a density of 1×103 cells/well. The final concentration of DMSO is 0.5% and the total volume is 100 µL/well. After 72 h incubation, Resazurin is added to each well (20 µL of 25 mg/100 mL stock in PBS) and incubated for an additional 4-6 h. To assess cell viability, fluorescence is quantified using an EnVision Multilabel Plate Reader at an excitation wavelength of 530 nm and emission of 590 nm. Triplicate data points are averaged to generate sigmoidal dose-response curves and determine IC50 values using XLfit curve fitting software. The IC50 is defined as the amount of compound required to decrease parasite or cell viability by 50% compared to those grown in the absence of the test compound. The MIC, defined as the lowest concentration of compound that completely inhibits visible parasite growth, is determined by visual inspection of 96-well plates after 48-72 h of incubation with the test compounds. To evaluate the effects of serum on trypanocidal activity, assays are performed in the presence of increasing concentration (2.5% to 50%) of fetal calf serum. The results are expressed as a fold-change in IC50 values relative to standard conditions (10% FCS) [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice, Rats and Monkeys[1]
Male CD-1 mice (~25 g), male Sprague-Dawley rats (~225 g), or male cynomolgus monkeys (~3-5 kg) are administered test article by either bolus intravenous injection (IV) or oral gavage. Male CD-1 mice, Sprague-Dawley rats, cynomolgus monkeys or male beagle dogs are administered a single oral dose of Acoziborole at a dose of 25 mg/kg (mouse, rat) or 10 mg/kg (monkey, dog). Blood samples are collected and analyzed.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.64%

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Acoziborole
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