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

SARS-CoV-2 Mpro-IN-5 是主要蛋白酶 (MPro) 和组织蛋白酶 L (CatL) 的双重抑制剂,IC50s 分别为 1800 nM 和 145 nM。SARS-CoV-2 Mpro-IN-5 对 SARS-CoV2 具有抗病毒活性。SARS-CoV-2 Mpro-IN-5 在表达 hACE2 的 A549 细胞中可阻断 SARS-CoV2 的复制,IC50 值为 14.7 nM。

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SARS-CoV-2 Mpro-IN-5 Chemical Structure

SARS-CoV-2 Mpro-IN-5 Chemical Structure

CAS No. : 3023276-79-8

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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 Mpro-IN-5 is a dual Inhibitor of Main Protease (MPro) and Cathepsin L (CatL), with IC50s of 1800 nM and 145 nM respectively. SARS-CoV-2 Mpro-IN-5 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-5 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 14.7 nM[1].

IC50 & Target

MPro/CatL[1]

体外研究
(In Vitro)

SARS-CoV-2 Mpro-IN-5 (SM142) blocks SARS-CoV2 replication in A549-hACE2 cells with IC50 value of 14.7 nM[1].
SARS-CoV-2 Mpro-IN-5 (0-50 μM, 24 h) cause cytotoxicity in A549-hACE2 cells[1].
SARS-CoV-2 Mpro-IN-5 inhibits OC-43 virus mRNA expression A549 cells[1].
SARS-CoV-2 Mpro-IN-5 inhibits SARS-CoV2 infection by inhibiting both MPro and CatL[1].

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

Cell Viability Assay[1]

Cell Line: A549-hACE2 cells
Concentration: 0, 0.1, 0.2, 2, 20, 50 μM
Incubation Time: 24 h
Result: Dose-dependently inhibited cell viability, reduce by 15% at 50 μM.
体内研究
(In Vivo)

SARS-CoV-2 Mpro-IN-5 (SM142) (10 mg/kg for i.n. or 25 mg/kg for i.p.) protects K18-ACE2 mice from SARS-CoV2-induced weight loss and lethality[1].
SARS-CoV-2 Mpro-IN-5 (3 mg/kg, i.v.) shows a half-life of 2.1 h and high clearance of 18490 mL/min/kg in in male C57Bl/6 mice[1].
SARS-CoV-2 Mpro-IN-5 (10 mg/kg, p.o.) shows oral bioavailability of 37.5%[1].

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

Animal Model: K18-hACE2 transgenic mice[1]
Dosage: 10 mg/kg (i.n.) or 25 mg/kg (i.p.)
Administration: Intranasal inhalation (i.n.), once daily for 3 days, prior to the infection; or Intraperitoneal injection (i.p.), twice daily for 5 days, postinfection administration.
Result: Prevented weight loss and prolonged survival.
分子量

638.73

Formula

C34H43FN4O7

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 Mpro-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 Mpro-IN-5
目录号:
HY-151901
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