2. Membrane Transporter/Ion Channel Anti-infection Immunology/Inflammation
  3. Sec61 SARS-CoV Interleukin Related
  4. KZR-8445 TFA

KZR-8445 TFA 是一种 Sec61 抑制剂。KZR-8445 TFA 可破坏分泌蛋白和膜蛋白的生物合成。KZR-8445 TFA 可抑制原代免疫细胞中促炎细胞因子的分泌。KZR-8445 TFA 能够阻断 SARS-CoV-2 的复制、病毒诱导的细胞毒性及刺突蛋白的生物合成。KZR-8445 TFA 在类风湿关节炎小鼠模型中可阻断疾病进展，且耐受性良好，无明显毒性。KZR-8445 TFA 可用于类风湿关节炎、病毒感染等疾病的研究。

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KZR-8445 TFA

KZR-8445 TFA Chemical Structure

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KZR-8445 TFA 相关抗体

Top Publications Citing Use of Products

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KZR-8445 TFA is a Sec61 inhibitor. KZR-8445 TFA disrupts the biosynthesis of secretory and membrane proteins. KZR-8445 TFA inhibits the secretion of proinflammatory cytokines in primary immune cells. KZR-8445 TFA blocks the replication of SARS-CoV-2, virus-induced cytotoxicity, and the biosynthesis of spike protein. KZR-8445 TFA blocks disease progression in a mouse model of rheumatoid arthritis with good tolerance and no obvious toxicity. KZR-8445 TFA can be used in the research of diseases such as rheumatoid arthritis and viral infection[1].

体外研究
(In Vitro)

KZR-8445 (0.1-1000 nM；24 h) TFA 可通过与 Sec61α 直接结合，在 HEK293 Flp-In T-REx 细胞中强效阻断 IL-2 和 TNFα 的分泌，但在表达 R66I Sec61α 突变体的细胞中活性降低[1]。
KZR-8445 (0.025-25000 nM; 24 h) TFA 可抑制受刺激的人外周血单个核细胞 (PBMCs) 和小鼠脾细胞中促炎细胞因子的分泌 (IC50 值达亚微摩尔级)，且在浓度高达 20 µM 时对细胞活力的影响极小[1]。
KZR-8445 TFA 可抑制 Vero E6 细胞中 SARS-CoV-2 的复制及刺突蛋白 (Spike protein) 的生物合成[1]。

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

KZR-8445 TFA 相关抗体:
体内研究
(In Vivo)

KZR-8445 (10-20 mg/kg；静脉注射；每周 3 次/每周 1 次；持续 2 周) TFA 可在类风湿关节炎小鼠模型中呈剂量依赖性阻断疾病进展[1]。

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

Animal Model: BALB/c (7- to 8-week-old female; rheumatoid arthritis)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.v.; thrice weekly (QODx3); 2 weeks; i.v.; weekly (QW); 2 weeks
Result: Blocked disease progression and produced a stronger anti-inflammatory effect than Dexamethasone (HY-14648).
Showed no significant toxicity, as evidenced by weight gain relative to vehicle-treated mice.
分子量

1197.98

Formula

C51H62BrF9N8O10
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

KZR-8445 TFA 相关分类

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  • 稀释计算器

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

质量   浓度   体积   分子量 *
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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)
× = ×
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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.

Keywords:

KZR-8445KZR8445KZR 8445Sec61SARS-CoVInterleukin RelatedSec61 complex, SecY, Sec61 channel SARS coronavirusILsignal peptidesSec61αcollagen antibodyT-cell acute lymphoblastic leukemia cellsmembrane protein biogenesispro-inflammatory cytokinesVero E6 cellsHEK293 Flp-In T-REx cellssecretory protein biogenesisSARS-CoV-2Inhibitorinhibitorinhibit

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