Acoziborole (SCYX-7158) 是一种安全有效的抗原虫剂，可用于人类非洲锥虫病 (HAT) 的研究。作用于 T. b. brucei S427 菌株，MIC 值为 0.6 µg/mL。

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.

Solid

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 inhibi

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,

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 125 mg/mL (340.51 mM)配制储备液