Cat. No.: HY-19910

Acoziborole

Name: Acoziborole
Brand: MedChemExpress
SKU: HY-19910
Price: 50.00 USD
Availability: InStock
Rating: 5 (3 reviews)

(Synonyms: SCYX-7158; AN5568)

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

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.

Purity : 99.96%
CAS No.: 1266084-51-8
Formula: C₁₇H₁₄BF₄NO₃
Molecular Weight:367.10

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Acoziborole Chemical Structure

CAS No.: 1266084-51-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Trypanosoma

All Parasite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Peritoneal macrophage	CC₅₀	>64 μM Compound: 1; AN556	Cytotoxicity against mouse primary peritoneal macrophages measured after 3 days by resazurin staining based fluorometric analysis Cytotoxicity against mouse primary peritoneal macrophages measured after 3 days by resazurin staining based fluorometric analysis	[PMID: 34711050]

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].

MedChemExpress (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 (t_1/2) of 26.6 h; systemic clearance (CL) of 0.089 L/h/kg; a volume of distribution (Vd_ss) of 1.69 L/kg and area under the concentration-time curve (AUC_{0-24 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 C_max 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 AUC_{0-24 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, C_max increases to 9.8 μg/mL and the AUC_{0-24 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), C_max increases approximately 2 fold more than that in mice (C_max=18.2 μg/mL) and AUC_{0-24 h}, and hence oral clearance, improves approximately 4 fold (AUC_{0-24 h} 291 h?μg/mL and CL/F=0.092 L/kg/h). The time to maximum concentration is similar to that in mice (t_max=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; Vd_ss of 0.656 L/kg and area under the concentration-time curve 78.8 h?μg/mL, and 94.4 for AUC_{0-24 h} and AUC_0-inf, respectively, following intravenous administration^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1266084-51-8
Appearance Solid
Molecular Weight 367.10
Formula C₁₇H₁₄BF₄NO₃
Color Off-white to light yellow
SMILES

O=C(NC1=CC=C2C(C)(C)OB(O)C2=C1)C3=CC=C(F)C=C3C(F)(F)F
Synonyms

SCYX-7158; AN5568
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

PLoS Pathog

2026 Mar 3;22(3):e1013764.
Biomed Chromatogr

LC-MS/MS determination of HY072808, a novel candidate for treating atopic dermatitis, and its active metabolite: Application to a first-in-human pharmacokinetic study. [Abstract]

2023 Feb;37(2):e5542. PMID: 36330676
bioRxiv

2025 Nov 27.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (272.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 5 mg/mL (13.62 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (13.62 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (13.62 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (293 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jacobs RT, et al. SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis. PLoS Negl Trop Dis. 2011 Jun;5(6):e1151. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7241 mL	13.6203 mL	27.2405 mL	68.1013 mL
	5 mM	0.5448 mL	2.7241 mL	5.4481 mL	13.6203 mL
	10 mM	0.2724 mL	1.3620 mL	2.7241 mL	6.8101 mL
	15 mM	0.1816 mL	0.9080 mL	1.8160 mL	4.5401 mL
	20 mM	0.1362 mL	0.6810 mL	1.3620 mL	3.4051 mL
	25 mM	0.1090 mL	0.5448 mL	1.0896 mL	2.7241 mL
	30 mM	0.0908 mL	0.4540 mL	0.9080 mL	2.2700 mL
	40 mM	0.0681 mL	0.3405 mL	0.6810 mL	1.7025 mL
	50 mM	0.0545 mL	0.2724 mL	0.5448 mL	1.3620 mL
	60 mM	0.0454 mL	0.2270 mL	0.4540 mL	1.1350 mL
	80 mM	0.0341 mL	0.1703 mL	0.3405 mL	0.8513 mL
	100 mM	0.0272 mL	0.1362 mL	0.2724 mL	0.6810 mL

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Acoziborole

Publications Citing Use of MedChemExpress (MCE) Acoziborole

All Parasite Isoforms