计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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.
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. IC 50 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 IC 50 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 IC 50 values for Acoziborole in these assays are all above 10 µM. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
规格
别名
阿克齐硼罗
规格或纯度
10mM in DMSO
英文名称
Acoziborole
生化机理
Acoziborole（SCYX-7158）是一种有效、安全且具有口服活性的抗原虫药物，可用于研究人类非洲锥虫病（HAT）。在布氏锥虫病 S427 菌株中，SCYX-7158 的 MIC 值为 0.6 µg/mL。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
裂解和多腺苷酸化特异性因子亚基抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
B1(C2=C(C=CC(=C2)NC(=O)C3=C(C=C(C=C3)F)C(F)(F)F)C(O1)(C)C)O
PubChem CID
分子量
367.10
技术文档
高级数据
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 J2613202 |
分析证书 | A656848 |
溶液计算器
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