1. Anti-infection
  2. SARS-CoV
  3. BZ-30

BZ-30 是一种具有口服活性的广谱 SARS-CoV-2 抑制剂。BZ-30 作用于病毒生命周期的早期阶段,可部分抑制内体进入过程并降低病毒复制水平。BZ-30 在经 SARS-CoV-2 攻毒的仓鼠模型中可降低病毒载量、改善肺部病理状况、降低肺体比。BZ-30 可用于新型冠状病毒肺炎的相关研究。

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BZ-30

BZ-30 Chemical Structure

CAS No. : 3028405-31-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BZ-30 is an orally active broad-spectrum SARS-CoV-2 inhibitor. BZ-30 acts on the early stage of the viral life cycle, can partially inhibit the endosomal entry process and reduce viral replication levels. BZ-30 reduces viral load, improves pulmonary pathological conditions, and decreases the lung-to-body weight ratio in hamster models challenged with SARS-CoV-2. BZ-30 can be used for research related to COVID-19[1].

体外研究
(In Vitro)

BZ-30 (0.15-5 μM) 在 5 μM 浓度下可使野生型 SARS-CoV-2 感染的 Vero E6 细胞中病毒 RNA 水平降低 ≥99%,呈现剂量依赖性抗病毒活性[1]
BZ-30 (24 h) 可强效抑制 Vero E6 细胞中野生型 SARS-CoV-2 的有效复制,其 IC50 为 0.65 μM[1]
BZ-30 (24 h) 在 Vero E6 细胞中作为新型冠状病毒关切变异株的广谱抑制剂,其 IC50 值范围为 0.51 μM (Beta 株) 至 12.37 μM (Omicron 株)[1]
BZ-30 可部分抑制 SARS-CoV-2 假病毒的内体进入;与 HEK293-ACE2/TMPRSS2 细胞中 50% 的抑制率相比,其在 HEK293-ACE2 细胞中的抑制作用更强 (最高可达 75%)[1]
BZ-30 (0-24 h) 在 Vero E6 细胞中作用于野生型 SARS-CoV-2 生命周期的早期阶段,在感染后 2 h 内给药时可抑制病毒复制[1]

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

药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax AUC0-last AUC0-∞ Bioavailability T1/2 Vd CL
Mice[1] 5 mg/kg i.v. / / 711.9 nM·h 877.6 nM·h / 3.9 h 8.43 L/kg 1.89 L/h/kg
Mice[1] 10 mg/kg p.o. 0.5 h 5003.8 nM 1759.4 nM·h 3029.1 nM·h 100 % / / /
体内研究
(In Vivo)

BZ-30 (15 mg/kg;腹腔注射;每日 2 次;感染后 8 小时开始给药,持续 4 天) 可使感染 SARS-CoV-2 的叙利亚金黄仓鼠体内病毒载量降低 64%,并改善其肺部病理状况[1]

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

Animal Model: Syrian Golden Hamsters (female, 6-8 weeks old, intranasally inoculated with 105 PFU of SARS-CoV-2)[1]
Dosage: 15 mg/kg
Administration: i.p.; twice daily; 4 days (starting 8 h post-infection)
Result: Reduced viral load by log10 0.44 TCID50 per mg lung, corresponding to a 64% reduction in viral load.
Significantly reduced the lung-to-body weight ratio.
Maintained body weight comparable to the positive control remdesivir.
Lowered the cumulative histopathological lung score from 14 to 3.
Showed minimal alveolar and epithelial cell degeneration, with only occasional peri-vascular and peri-bronchiolar focal inflammatory cell infiltration.
分子量

337.26

Formula

C14H13F6N3

CAS 号
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
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  • 稀释计算器

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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.

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产品名称:
BZ-30
目录号:
HY-183185
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