1. Anti-infection Metabolic Enzyme/Protease
  2. Virus Protease SARS-CoV Cathepsin
  3. Olgotrelvir

Olgotrelvir (STI-1558) 是一种有口服活性的冠状病毒主蛋白酶 (Mpro) 和人细胞组织蛋白酶 (Cathepsin L) 的双重抑制剂。Olgotrelvir 在全血和/或血浆中很容易转化为其活性形式 AC1115。Olgotrelvir 可以有效抑制 SARS-CoV-2 复制和进入宿主细胞。

该游离形式化合物不稳定,推荐具有相同生物学活性的稳定盐形式 Olgotrelvir sodium

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Olgotrelvir Chemical Structure

Olgotrelvir Chemical Structure

CAS No. : 2763596-71-8

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Olgotrelvir 的其他形式现货产品:

Customer Review

Other Forms of Olgotrelvir:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Olgotrelvir (STI-1558) is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir can effectively inhibit both SARS-CoV-2 replication and entry into host cells[1][2].

体外研究
(In Vitro)

Olgotrelvir (0-100 μM;每隔一天更换一次,持续 3 至 5 天) 在感染了 SARS-CoV-2 VOC (包括 WA-1、Alpha、Beta、Delta、Lambda 和 Gamma 变体) 的 Vero E6 细胞中均显示出抗病毒活性,平均 EC50 值为 0.28 至 4.26 μM[2]

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

药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Cynomolgus Monkey 84 mg/kg p.o. AUC0-inf 90900 ng·h/mL
Dog 12.5 mg/kg p.o. AUC0-inf 15200 ng·h/mL
Dog 25 mg/kg p.o. AUC0-inf 30500 ng·h/mL
Dog 50 mg/kg p.o. AUC0-inf 61800 ng·h/mL
Mice 300 mg/kg p.o. AUC0-inf 8030 ng·h/mL
Mice 500 mg/kg p.o. AUC0-inf 12400 ng·h/mL
Rat 100 mg/kg p.o. AUC0-inf 2000 ng·h/mL
Rat 200 mg/kg p.o. AUC0-inf 3580 ng·h/mL
Rat 500 mg/kg p.o. AUC0-inf 8050 ng·h/mL
Cynomolgus Monkey 84 mg/kg p.o. T1/2 4.84 hr
Dog 12.5 mg/kg p.o. T1/2 4.01 hr
Dog 25 mg/kg p.o. T1/2 3.76 hr
Dog 50 mg/kg p.o. T1/2 3.51 hr
Mice 300 mg/kg p.o. T1/2 1.58 hr
Mice 500 mg/kg p.o. T1/2 1.9 hr
Rat 100 mg/kg p.o. T1/2 1.48 hr
Rat 200 mg/kg p.o. T1/2 1.84 hr
Rat 500 mg/kg p.o. T1/2 2.03 hr
Cynomolgus Monkey 84 mg/kg p.o. Cmax 18800 ng/mL
Dog 12.5 mg/kg p.o. Cmax 3600 ng/mL
Dog 25 mg/kg p.o. Cmax 7080 ng/mL
Dog 50 mg/kg p.o. Cmax 13200 ng/mL
Mice 300 mg/kg p.o. Cmax 7290 ng/mL
Mice 500 mg/kg p.o. Cmax 10600 ng/mL
Rat 100 mg/kg p.o. Cmax 1200 ng/mL
Rat 200 mg/kg p.o. Cmax 2650 ng/mL
Rat 500 mg/kg p.o. Cmax 6460 ng/mL
Cynomolgus Monkey 84 mg/kg p.o. Tmax 2.7 hr
Dog 12.5 mg/kg p.o. Tmax 2.0 hr
Dog 25 mg/kg p.o. Tmax 1.5 hr
Dog 50 mg/kg p.o. Tmax 2.0 hr
Mice 300 mg/kg p.o. Tmax 0.25 hr
Mice 500 mg/kg p.o. Tmax 0.25 hr
Rat 100 mg/kg p.o. Tmax 0.17 hr
Rat 200 mg/kg p.o. Tmax 0.083 hr
Rat 500 mg/kg p.o. Tmax 0.083 hr
Cynomolgus Monkey 84 mg/kg p.o. F 48.3 %
Dog 12.5 mg/kg p.o. F 83.1 %
Dog 25 mg/kg p.o. F 83.5 %
Dog 50 mg/kg p.o. F 84.7 %
Mice 300 mg/kg p.o. F 5.06 %
Mice 500 mg/kg p.o. F 4.69 %
Rat 100 mg/kg p.o. F 2.94 %
Rat 200 mg/kg p.o. F 2.62 %
Rat 500 mg/kg p.o. F 2.36 %
体内研究
(In Vivo)

Olgotrelvir (400-1000 mg/kg;病毒接种后立即口服,每日两次) 在被感染了 SARS-CoV-2 WA-1 病毒的 K18-hACE2 转基因小鼠中具有抗病毒活性,并可减轻肺部病理[2]

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

Animal Model: K18-hACE2 transgenic mice (express human ACE2 in the lung epithelia, including airway epithelia, under the control of the human keratin 18 promoter)[2]
Dosage: 400, 500, 1000 mg/kg
Administration: Oral gavage (p.o.); twice a day immediately after SARS-CoV-2 WA-1 strain inoculation
Result: Prevented weight loss.
On day 5 post infection, virus was below the detectable level in the lungs.
Pathological changes caused by SARS-CoV-2 infection were relieved.
At a dose of 1000 mg/kg at the 12th hour post-infection resulted in significant reduction of viral RNA shedding and prevention of the body weight loss.
Blocked pro-inflammatory cytokine (IL-6, TNF-α, GM-CSF) release at 400 mg/kg dosage.
Clinical Trial
分子量

494.56

同用名

STI-1558

Formula

C22H30N4O7S

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
  • 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.

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Olgotrelvir
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HY-156655
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