1. Anti-infection Metabolic Enzyme/Protease
  2. SARS-CoV Virus Protease Ser/Thr Protease
  3. TMP1

TMP1 是一种具有口服活性的 M pro (IC50 = 312.5  nM)/TMPRSS2 (IC50 = 1.28 μM, KD = 10.10 μM) 双特异性抑制剂。TMP1 在体外对不同的 SARS-CoV-2 变体表现出广谱保护作用。TMP1 在体内对高致病性冠状病毒 (SARS-CoV-1SARS-CoV-2 和 MERS-CoV) 具有交叉保护作用,并能有效阻断 SARS-CoV-2 的传播。TMP1 能够抑制 Nivolumab (HY-P9903) 耐药的 SARS-CoV-2 逃逸突变体的感染。TMP1 可用于冠状病毒研究。

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

TMP1

TMP1 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TMP1 is an orally active bispecific inhibitor of M pro (IC50 = 312.5 nM)/TMPRSS2 (IC50 = 1.28 μM, KD = 10.10 μM). TMP1 exhibits broad protection against different SARS-CoV-2 variants in vitro. TMP1 cross-protects against highly pathogenic coronaviruses (SARS-CoV-1, SARS-CoV-2, and MERS-CoV) in vivo and effectively blocks the transmission of SARS-CoV-2. TMP1 can inhibit infection by SARS-CoV-2 escape mutants that are resistant to Nivolumab (HY-P9903). TMP1 can be used in coronavirus research[1].

体外研究
(In Vitro)

TMP1 (48 小时) 在 VeroE6-TMPRSS2 细胞中对野生型 SARS-CoV-2 及其他变异株 (VOC) (包括 Alpha、Beta、Delta 和 Omicron (BA.1 和 JN.1)) 无细胞毒性,在感染了 SARS-CoV-2 Omicron 亚型 JN.1 和 KP.2 的人鼻上皮细胞 (ALI-hNEC) 中,降低病毒基因拷贝数和病毒滴度[1]
TMP1 (0-20 µM,24 小时) 在 2 µM P-gp 抑制剂 CP-100356 (HY-108347) 存在下,可降低 VeroE6、VeroE6-TMPRSS2 和 LLC-MK2 细胞中的病毒负担和感染性子代病毒滴度[1]
TMP1 (0-50 µM,24-48 小时) 可抑制季节性 HCoV (HCoV-HKU1、-OC43、-NL63 和 -229E) 的复制,EC50 范围为 0.31 至 2.60 µM,可交叉保护对抗高致病性冠状病毒 SARS-CoV-1 和 MERS-CoV,EC50 分别为 0.55 和 5.26 µM[1]
TMP1 (1-50 µM) 可抑制由 SARS-CoV-2 野生型刺突蛋白介导的 TMPRSS2 依赖性细胞间融合[1]
TMP1 抑制重组 SARS-CoV-2、SARS-CoV-1 和 MERS-Co V的 M pro,IC50 分别为 0.313、0.516 和 74.6 µM[1]
TMP1 (0-50 µM) 可降低 TMPRSS-2 缺陷型 VeroE6 细胞中 SARS-CoV-2、SARS-CoV-1 和 MERS-CoV 的复制[1]
TMP1 在 rSARS-CoV-2 NSP5-E166V 感染的 Calu3 细胞中可减少 rSARS-CoV-2 NSP5-E166V 的细胞内病毒基因拷贝数, EC50 为 0.449 µM [1]

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

体内研究
(In Vivo)

TMP1 (100 mg/kg,口服,每日两次,4 天) 在感染 SARS-CoV-2 的杂合子 K18-hACE2 C57BL/6 J 小鼠中可降低受感染小鼠呼吸道中的病毒负担,改善感染相关组织病理,从而提高总体生存率[1]
TMP1 (90 mg/kg,口服,一次) 在 PFU SARS-CoV-2 Delta 感染的金黄叙利亚仓鼠模型中可对抗人类上呼吸道上皮中普遍存在的 Omicron 谱系,并可有效减弱 SARS-CoV-2 的传播[1]
TMP1 (100-150 mg/kg,口服,每日两次,4 天) 在 SARS-CoV-1 感染的杂合子小鼠和 MERS-CoVMA 感染的杂合子 hDPP4-KI 小鼠中可提供广谱抗病毒保护[1]
TMP1 (100 mg/kg,口服,每日两次,4 天) 与 M pro 的相互作用机制与 NRV 不同,因此在感染 rSARS-CoV-2 NSP5-E166V 的杂合子 K18-hACE2 C57BL/6 J 小鼠中仍保留了敏感性[1]

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

Animal Model: SARS-CoV-2-infected (500-1250 PFU) heterozygous K18-hACE2 C57BL/6 J mice (6-12-week-old)[1]
Dosage: 100 mg/kg
Administration: o.p., twice per day, 4 days
Result: Could be maintained at 11.1-, 11.4- and 6.5-fold higher than its in vitro EC50 of SARS-CoV-2 Delta.
Suppressed SARS-CoV-2 infection, reduced viral burdens in the lung tissues, the expression of N protein, alleviated or absent loss of epithelium integrity, septal inflammation, alveoli deformation, and submucosal inflammatory infiltrations.
Delayed onset of death, rescued the survival rate, lowered viral gene copies by 7.3- and 9.2-fold in the nasal turbinate and lung tissues, respectively.
Animal Model: SARS-CoV-2 Delta-infected 2000 PFU) golden syrian hamsters (8-10-week-old) model[1]
Dosage: 90  mg/kg
Administration: o.p., once
Result: Reduced viral gene copies in the exposed nasal canal, infectious virus titers, viral load in lung tissue, and viral N protein expression, alleviated the massive inflammatory infiltration in the alveolar septa and alveolar deformation.
Animal Model: SARS-CoV-1-infected (500 PFU) heterozygous K18-hACE2 C57BL/6 J mice (6-12-week-old)[1]
Dosage: 100 mg/kg
Administration: o.p., twice per day, 4 days
Result: Reduced viral load and SARS-CoV-1 nucleocapsid protein expression in nasal turbinates and lung tissues, titers of infectious viral progeny in the lungs, and alleviated loss of nasal mucosal epithelial integrity and alveolar damage.
Animal Model: MERS-CoVMA-infected (500 PFU) heterozygous hDPP4-KI C57BL/6 J mice (6-12-week-old)[1]
Dosage: 150 mg/kg
Administration: o.p., twice per day, 4 days
Result: Suppressed MERS-CoVMA replication in both nasal turbinates and lungs, decreased infectious viral titres and expression of MERS-CoVMA N protein in the nasal turbinate and lung tissues. Alleviated virus-induced epithelial damage in the nasal turbinate and reduced alveolar destruction.
Animal Model: RSARS-CoV-2 NSP5-E166V-infected heterozygous K18-hACE2 C57BL/6 J mice (6-12-week-old)[1]
Dosage: 100 mg/kg
Administration: o.p., twice per day, 4 days
Result: Reduced infectious virus titers in nasal turbinates and lung tissues, viral antigens in nasal turbinates, N protein expression in infected lung tissue samples, and ameliorated virus-induced pathological changes.
分子量

718.21

Formula

C36H43ClF3N5O5

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
  • 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.

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:
TMP1
目录号:
HY-175344
需求量: