1. Anti-infection
  2. SARS-CoV
  3. SARS-CoV-2 3CLpro-IN-5

SARS-CoV-2 3CLpro-IN-5 是 3CLpro 的共价抑制剂。SARS-CoV-2 3CLpro-IN-5 对 3C 样蛋白酶3CLpro 具有抑制活性,IC50 值为 3.8 nM。SARS-CoV-2 3CLpro-IN-5 具有 9.0% 的口服生物利用度 (BA)。SARS-CoV-2 3CLpro-IN-5 可用于 COVID-19 的研究。

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SARS-CoV-2 3CLpro-IN-5 Chemical Structure

SARS-CoV-2 3CLpro-IN-5 Chemical Structure

CAS No. : 2913186-57-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CLpro). SARS-CoV-2 3CLpro-IN-5 has inhibitory activity for 3CLpro with an IC50 value of 3.8 nM. SARS-CoV-2 3CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-2 3CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19)[1].

IC50 & Target

IC50: 3.8 nM (3CLpro)[1].
EC50 for SARS-CoV-2 strains: 13.8 nM (α), 7.57 nM (δ), 9.01 nM (Om BA.1) and 17.1 nM (Om BA.2) [1].
EC50: 59.3 nM (SARS-CoV in 293TAT cells); 4.72 nM (MERS-CoV in 293TDPP4 cells); 1.67 nM (HCoV-OC43 in 293TAT cells)[1].

体外研究
(In Vitro)

SARS-CoV-2 3CLpro-IN-5 has inhibitory activity for 3CLpro with an IC50 value of 3.8 nM[1].
SARS-CoV-2 3CLpro-IN-5 has antiviral activity in 293TAT cells againsts various SARS-CoV-2 strains α, δ, Om BA.1 and Om BA.2 with EC50 values of 13.8 nM, 7.57 nM, 9.01 nM and 17.1 nM, respectively[1].
SARS-CoV-2 3CLpro-IN-5 has antiviral activity against various coronaviruses SARS-CoV (293TAT cells), MERS-CoV (293TDPP4 cells) and HCoV-OC43 (293TAT cells) with EC50 values of 59.3 nM, 4.72 nM and 1.67 nM, respectively[1].

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

体内研究
(In Vivo)

SARS-CoV-2 3CLpro-IN-5 (oral, i.v.; 10, 100 mg/kg) has strong antiviral activity and favorable pharmacokinetic properties[1].

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

Animal Model: mice[1]
Dosage: 10, 100 mg/kg
Administration: oral (100 mg/kg) and intravenous (10 mg/kg) administration
Result: Showed the plasma concentration was 15.2 μM after 1 h and decreased to 0.40 μM over 6 h after oral administration (100 mg/kg) .
Showed the plasma concentration reached 9.3 μM after 1 h and decreased to 0.33 μM after 6 h in intravenous administration (10 mg/kg) .
Had approximately 9.0% estimated bioavailability (BA).
分子量

497.92

Formula

C22H26ClF2N5O4

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

SARS-CoV-2 3CLpro-IN-5 相关分类

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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:
SARS-CoV-2 3CLpro-IN-5
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HY-151535
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