2. Anti-infection
  3. Virus Protease
  4. BFB78

BFB78 是一种可穿过血脑屏障的 nsP2 蛋白酶 (nsP2 protease) 抑制剂。BFB78 强效且广谱地抑制多种甲病毒的纯化 nsP2 蛋白酶，其 IC50 值范围为 21.6 nM (马亚罗病毒；MAYV) 至 130.7 nM (基孔肯亚病毒；CHIKV)。BFB78 可阻断细胞培养体系中的病毒复制，并降低小鼠脑内的病毒滴度。BFB78 可用于委内瑞拉马脑炎病毒感染 (VEEV) 的相关研究。

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BFB78

BFB78 Chemical Structure

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BFB78 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BFB78 is a blood-brain barrier-permeable nsP2 protease inhibitor. BFB78 potently and broadly inhibits the purified nsP2 proteases of various alphaviruses, with IC50 values ranging from 21.6 nM (Mayaro virus; MAYV) to 130.7 nM (Chikungunya virus; CHIKV). BFB78 blocks viral replication in cell culture systems and reduces viral titers in the brains of mice. BFB78 can be used in studies related to Venezuelan equine encephalitis virus (VEEV) infection[1].

体外研究
(In Vitro)

BFB78 (49 h) 可抑制培养细胞中 WEEV、VEEV 和 MAYV 的病毒复制，其 EC50 值分别为 1.1 μM、1.6 μM和 1.2 μM[1]。
BFB78 (72 h) 在 Hep G2 细胞、SVG p12 星形胶质细胞和 Vero 76 细胞中表现出低细胞毒性，所有受试细胞系的 CC50 值均 > 32 μM[1]。
BFB78 (2 μM; 0-120 min) 在小鼠和人源肝脏 S9 组分及微粒体中具有极高的代谢稳定性，在所有受试代谢体系中的半衰期均> 120 min[1]。
BFB78 (5 μM) 具有穿过 MDCKII 细胞单层的高渗透性，且在 MDR1-MDCKII 细胞中被 P-gp 外排的水平较低[1]。

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

BFB78 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax T1/2 AUC0-∞ Vz CL MRT
Mice[1] 40 mg/kg p.o. 1353 ng/mL 133 min 175098 min·ng/mL 43711 mL/kg 228 mL/min/kg 166 min
体内研究
(In Vivo)

BFB78 (50 mg/kg；腹腔注射；每日 2 次; 共 10 天) 在致死性 VEEV TC-83 小鼠模型中可实现 100%的治疗效果，平均脑病毒滴度降低超过 4 log10[1]。

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

Animal Model: C3H/HeN (Charles River, Strain 025; intranasally infected with VEEV TC-83 at 1×107 PFU)[1]
Dosage: 50 mg/kg
Administration: i.p.; twice daily; until euthanasia criteria met or day 10 post-infection
Result: Achieved 100% survival of treated mice until euthanasia on day 11 post-infection.
Reduced viral titers in mouse brain tissue by an average of more than 4 log10 compared with vehicle-treated animals.
Mitigated weight loss in infected mice relative to vehicle-treated and comparator-treated animals.
分子量

318.39

Formula

C16H18N2O3S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BFB78 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BFB78BFB 78BFB-78Virus Proteasemouse liver phase I metabolic enzymesCHIKVblood-brain barriermouse liver phase II metabolic enzymeshuman liver phase II metabolic enzymesalphaviruseshuman liver phase I metabolic enzymesnsP2 proteasevenezuelan equine encephalitis viral infectionMAYVInhibitorinhibitorinhibit

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