2. Anti-infection
  3. Virus Protease SARS-CoV
  4. MR1-114

MR1-114 是一种具有口服活性 SARS-CoV-2 木瓜样蛋白酶 (PLpro) 抑制剂，IC50 为 0.037 μM。MR1-114 可作为一种广谱抑制剂，对 SARS-CoV-2 Delta、Omicron B.1.1.529 和 Omicron BA.5 变异株保持亚微摩尔级活性，其 EC50 值分别为 0.18 μM、0.39 μM 和 0.20 μM。MMR1-114 可用于新型冠状病毒肺炎 (SARS-CoV-2 感染) 的研究。

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MR1-114

MR1-114 Chemical Structure

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MR1-114 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

MR1-114 is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor with an IC50 of 0.037 μM. As a broad-spectrum inhibitor, MR1-114 maintains submicromolar activity against SARS-CoV-2 Delta, Omicron B.1.1.529 and Omicron BA.5 variants, with EC50 values of 0.18 μM, 0.39 μM and 0.20 μM, respectively. MR1-114 can be used for the research of coronavirus disease 2019 (SARS-CoV-2 infection)[1].

体外研究
(In Vitro)

MR1-114 可强效抑制纯化的重组 SARS-CoV-2 PLpro，其 IC50 为 0.037 μM[1]。
MR1-114 (48 h) 在 A549-hACE2 细胞中表现出低细胞毒性，其 CC50 为 34.54 μM[1]。
MR1-114 (1-10 μM; 1 h) 可强效抑制 A549-hACE2 细胞中 SARS-CoV-2 WA1 的复制，在 1 μM 浓度下使病毒载量降低 1.54 log，在 10 μM 浓度下降低 6.41 log[1]。
MR1-114 (2 h) 可作为一种广谱抑制剂，在 A549-hACE2 细胞中对 SARS-CoV-2 Delta、Omicron B.1.1.529 和 Omicron BA.5 变异株保持亚微摩尔级活性，其 EC50 值分别为 0.18 μM、0.39 μM 和 0.20 μM[1]。

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

MR1-114 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUCinf CL_obs Vss_obs Bioavailability
Mice[1] 10 mg/kg p.o. 2.11 h 6091 (plasma) ng·h/mL / / 60.2 %
Mice[1] 1 mg/kg i.v. 1.80 h 1012 (plasma) ng·h/mL 16.7 mL/min/kg 2.33 L/kg /
Rat[1] 10 mg/kg p.o. 2.78 h 10954 (plasma) ng·h/mL / / 71.2 %
Rat[1] 1 mg/kg i.v. 3.00 h 1538 (plasma) ng·h/mL 11.0 (plasma) mL/min/kg 2.40 L/kg /
体内研究
(In Vivo)

MR1-114 (100-150 mg/kg；口服；每日 2 次；连续 5 天) 在感染 SARS-CoV-2 WA1 的 K18-ACE2 小鼠中可预防疾病相关的体重下降，且使肺部病毒复制水平降低[1]。

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

Animal Model: B6.Cg-Tg(K18-ACE2)2Prlmn/J (female, 6−8 weeks of age, SARS-CoV-2 WA1 intranasal challenge)[1]
Dosage: 100 mg/kg; 150 mg/kg
Administration: p.o.; twice daily; 5 days
Result: Maintained body weight percentages comparable to mock-infected and nirmatrelvir-treated groups, preventing disease-associated weight loss.
Produced a statistically significant ~1 log decrease in lung viral titers relative to vehicle control at 150 mg/kg, comparable to Nirmatrelvir (1000 mg/kg, twice daily).
分子量

521.66

Formula

C31H35N7O
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

MR1-114 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:

MR1-114Virus ProteaseSARS-CoVSARS coronavirusK18-ACE2 miceA549-hACE2 cellsSARS-CoV-2 papain-like proteaseVal70Ub pocketBL2 grooveOmicron BA.5PLproDeltacovid-19SARS-CoV-2 variantsInhibitorinhibitorinhibit

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目录号：
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