- ￥1580 - 5790
- Solarbio
- 北京
- IA2080
- 2026年04月15日
企业认证
相关产品推荐更多 >
万千商家帮你免费找货
0 人在求购买到急需产品
- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Acoziborole
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1266084-51-8
- 规格：
10mg/5mg/1mg
| 规格： | 10mg | 产品价格： | ￥5790.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥3490.0 |
| 规格： | 1mg | 产品价格： | ￥1580.0 |
是一种具有有效抗锥虫活性的化合物
| 基本信息 | |
| CAS | No.1266084-51-8 |
| 英文名称 | Acoziborole |
| 别名 | SCYX-7158;AN5568 |
| 分子式 | C17H14BF4NO3 |
| 分子量 | 367.1 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES | O=C(NC1=CC=C2C(C)(C)OB(O)C2=C1)C3=CC=C(F)C=C3C(F)(F)F |
| 靶点 | Parasite |
| 通路 | Anti-infection |
| 背景说明 | Acoziborole是一种具有有效抗锥虫活性的化合物。 |
| 生物活性 | 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]. |
| 细胞实验 | 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 hμg/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 hμg/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 hμg/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 hμg/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 hμg/mL，and 94.4 for AUC0-24 h and AUC0-inf，respectively，following intravenous administration[1]. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
风险提示：丁香通仅作为第三方平台，为商家信息发布提供平台空间。用户咨询产品时请注意保护个人信息及财产安全，合理判断，谨慎选购商品，商家和用户对交易行为负责。对于医疗器械类产品，请先查证核实企业经营资质和医疗器械产品注册证情况。
文献和实验相关实验
侵袭性真菌感染(Invasive Fungal Infection, IFI)是接受联合化疗及 造血干细胞 移植(Hematopoietic stem cell transplantation, HSCT)患者的严重并发症，其中侵袭性曲霉菌病(Invasive Aspergillosis , IA)是较为常见的一种，且发生率逐年上升，1在血液病和HSCT患者中病死率高达50%-90%。2造成高病死率的主要原因是IA 早期诊断困难，使得治疗延迟。3 以往常用的诊断IA
细胞起约束作用。 （一）Mφ、T、B细胞相互作用过程中的MHC约束性 Rosenthal和Shevach(1973)首先在豚鼠中观察到T细胞只能被具有相同MHc I区基因（Ⅱ类基因）的抗原提呈细胞所激活（表6-13）。同年Katz等人也发现Th与B细胞相互作用时，只有在两者MHc I区（Ⅱ类基因）相同的条件才会出现协作应（表6-14）。 表6-13 豚鼠T细胞对胸腺信赖抗原的免疫应答中Mφ提呈抗原与Ia抗原的关系 OVA预处理T细胞 OVA加Mφ DNA合成的增加
技术资料暂无技术资料 索取技术资料
IA2080 Acoziborole 抗感染 索莱宝
￥1580 - 5790
