2. Anti-infection
  3. SARS-CoV Virus Protease
  4. YL1004

YL1004 是一种强效、选择性且口服有效的非共价抑制剂，可抑制 SARS-CoV-2 木瓜蛋白酶样蛋白酶 (PLpro)。YL1004 对 PLpro 的 IC50 为 17.5 nM，Ki 为 2.3 nM，体外抗 SARS-CoV-2 的 EC50 为 0.08 μM-1.37 μM。YL1004 可抑制 PLpro 的蛋白水解活性，并阻断其去泛素化和去 ISG 化作用，以恢复宿主固有抗病毒免疫信号通路。YL1004 可抑制 SARS-CoV-2 野生株、Delta 株、Omicron 变异株以及耐奈玛特韦毒株的复制。YL1004 可用于新型冠状病毒肺炎 (SARS-CoV-2 感染) 的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

YL1004

YL1004 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

YL1004 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

YL1004 is a potent, selective and orally active noncovalent inhibitor of SARS-CoV-2 papain-like protease (PLpro). YL1004 shows an IC50 of 17.5 nM and a Ki of 2.3 nM against PLpro, with an in vitro anti-SARS-CoV-2 EC50 of 0.08 μM-1.37 μM. YL1004 suppresses the proteolytic activity of PLpro and blocks its deubiquitinating and deISGylating effects to restore host innate antiviral immune signaling. YL1004 inhibits the replication of wild-type, Delta, Omicron variants and nirmatrelvir-resistant strains of SARS-CoV-2. YL1004 can be used for the research of COVID-19 (SARS-CoV-2 infection)[1].

体外研究
(In Vitro)

YL1004 (室温下预孵育 10 分钟) 可抑制 SARS-CoV-2 PLpro 介导的多蛋白切割，其 IC50 为 17.5 nM，Ki 为 2.3 nM；可抑制 SARS-CoV-2 PLpro 介导的去泛素化作用，IC50 为 22.9 nM，Ki 为 4.2 nM；还可抑制 SARS-CoV-2 PLpro 介导的去 ISG 化作用，IC50 为 43.6 nM，Ki 为 39.3 nM[1]。
YL1004 (孵育 72 h) 在哺乳动物细胞系中表现出低细胞毒性，在 VeroE6 细胞中的 CC50 为 226.90 μM，在 Calu3 细胞中的 CC50 为 296.33 μM[1]。
YL1004 可直接与 SARS-CoV-2 PLpro 结合，这一点通过 DSF 实验中 18.07°C 的 ΔTm 得到证实[1]。
YL1004 (0.001-10 μM; 36 h) 可在 HEK293T 细胞中剂量依赖性地抑制 SARS-CoV-2 PLpro 介导的去泛素化作用[1]。
YL1004 (0.1-10 μM; co-treated with PLpro following 48 h IFN-α stimulation) 可在 IFN-α 刺激的 A549 细胞中呈剂量依赖性抑制 SARS-CoV-2 PLpro 介导的去 ISG 化修饰[1]。
YL1004 (0.002-10 μM; co-treated with TNF-α (HY-P7058) stimulation) 可恢复表达 PLpro 的 HEK293T 细胞中由 TNF-α 诱导的 NF-κB 激活，其 EC50 为 44.1 nM；同时可恢复 ISRE 激活，EC50 为 265.3 nM[1]。
YL1004 (0.002-10 μM; co-treated with poly (I:C) (HY-107202) stimulation) 可恢复表达 PLpro 的 HEK293T 细胞中由 poly (I:C) 诱导的 IFNB1 与 IRF3 激活，其 EC50 值分别为 26.5 nM 和 206.9 nM[1]。
YL1004 (在 poly (I:C) 刺激同时给药后 18-24 h) 可恢复经 poly (I:C) 刺激的 HEK293T 细胞中被 PLpro 抑制的、参与固有免疫、自噬及线粒体应激反应的基因的转录水平[1]。
YL1004 (0.039-10 μM; 22 h for wildtype/Delta/JN.1, 46 h for KP.3/NSP5-E166V) 可剂量依赖性降低受感染 Calu3 细胞中的 SARS-CoV-2 sgE RNA 水平[1]。
YL1004 (感染后野生型/Delta 株作用 48 h，JN.1/KP.3/NSP5-E166V 株作用 72 h) 可强效抑制具有感染性的 SARS-CoV-2 复制，在野生型、Delta、奥密克戎 JN.1、奥密克戎 KP.3 以及耐奈玛特韦的 NSP5-E166V 重组毒株中，其 EC50 值范围为 0.08 μM 至 1.37 μM[1]。

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

YL1004 相关抗体:

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 0.01, 0.05, 0.1, 0.25, 0.5, 1, 10 μM
Incubation Time: 36 h
Result: Restored ubiquitinated protein levels in a dose-dependent manner.
Showed greater potency than 10 μM of a reference compound at suppressing PLPRO-mediated deubiquitination when used at 1 μM.

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 0.1, 1, 10 μM
Incubation Time: with or without IFN-α for 48 h
Result: Reversed PLPRO-mediated reduction of ISG15-conjugated proteins in a dose-dependent manner.

Real Time qPCR[1]

Cell Line: Calu3 cells infected with SARS-CoV-2 wildtype, Delta, Omicron JN.1, Omicron KP.3, and NSP5-E166V recombinant strains
Concentration: 0.039, 0.16, 0.63, 2.5, 110 μM
Incubation Time: 24 h (WT, Delta, JN.1); 48 h (KP.3, NSP5-E166V mutant)
Result: Dose-dependently reduced SARS-CoV-2 sgE RNA levels; inhibited replication of WT, Delta, Omicron JN.1/KP.3 and nirmatrelvir-resistant strain.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t Bioavailability
Mice[1] 100 mg/kg p.o. 79818.17 μg/L·h 61.2 %
Rat[1] 10 mg/kg p.o. 14723.3 μg/L·h /
体内研究
(In Vivo)

YL1004 (100 mg/kg; p.o.; twice per day) 可显著降低感染 Omicron JN.1 的 K18-hACE2 小鼠的病毒载量、病毒抗原水平及病理损伤，与溶媒对照组相比，其肺组织病毒 RNA 水平降低 26.1 倍，肺组织感染滴度降低 13.4 倍[1]。
YL1004 (100 mg/kg; p.o.; twice per day) 于攻毒后 1 小时开始给药，可使 SARS-CoV-2 Delta 株攻毒的 K18-hACE2 小鼠获得 100%的存活率并减轻体重下降[1]。

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

Animal Model: K18-hACE2 transgenic (8-12-week-old; male and female; intranasal inoculation with SARS-CoV-2 Omicron JN.1)[1]
Dosage: 100 mg/kg
Administration: p.o.; twice per day
Result: Decreased viral sgE RNA loads in nasal turbinates by 3.6-fold compared to vehicle controls.
Decreased viral sgE RNA loads in lung tissues by 26.1-fold compared to vehicle controls.
Lowered infectious viral titers in nasal turbinates by 21-fold compared to vehicle controls.
Lowered infectious viral titers in lung tissues by 13.4-fold compared to vehicle controls.
Rarely detected viral antigen in treated mouse lungs.
Significantly alleviated virus-induced pathological changes, with only mild alveolar deformation observed.
Animal Model: K18-hACE2 transgenic (8-12-week-old; female; intranasal inoculation with SARS-CoV-2 Delta)[1]
Dosage: 100 mg/kg
Administration: p.o.; twice per day
Result: Reduced body weight loss significantly compared to vehicle controls.
Achieved 100% survival (10/10 mice) at 14 days post-infection, compared to 10% survival (1/10 mice) in vehicle controls.
分子量

527.66

Formula

C31H37N5O3
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

YL1004 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:

YL1004YL 1004YL-1004SARS-CoVVirus ProteaseSARS coronavirushuman deubiquitinasesA549 cellsHEK293T cellsSARS-CoV-2 wildtypeOmicronSARS-CoV-2 papain-like proteaseSARS-CoV-2 PLpronirmatrelvir-resistant Mpro E166V strainsCalu3 cellsDeltaInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
YL1004
目录号：
HY-181661
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z