2. Anti-infection
  3. SARS-CoV
  4. Leritrelvir

Leritrelvir  (Synonyms: RAY1216)

目录号: HY-153121
产品使用指南

摩尔计算器

Leritrelvir (RAY1216) 是一种具有口服活性的 SARS-CoV-2 主要蛋白酶慢紧抑制剂，Ki 为 8.6 nM。

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Leritrelvir Chemical Structure

Leritrelvir Chemical Structure

CAS No. : 2923310-64-7

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规格 价格 是否有货
1 mg ￥3900
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5 mg ￥9800
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Customer Review

Leritrelvir 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

Leritrelvir (RAY1216) is an orally active SARS-CoV-2 main protease slow-tight inhibitor with a Ki of 8.6 nM[1].

IC50 & Target

Ki: 8.6 nM (SARS-CoV-2 main protease)[1]
体外研究
(In Vitro)

Leritrelvir (RAY1216) 的药物靶向停留时间为 104 分钟[1]。
Leritrelvir 通过 α-ketoamide warhead 共价连接到催化的 Cys145 上[1]。
Leritrelvir (0-1000 nM; 72 h) 显示出对 SARS-CoV-2 野生型祖先株和变异株的抗病毒活性[1]。

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

Leritrelvir 相关抗体:

Cell Viability Assay[1]

Cell Line: Vero E6 cells inoculated with SARS-CoV-2 WT, Alpha, Beta, Delta, Omicron BA.1 and Omicron 247 BA.5 strains
Concentration: 0-1000 nM
Incubation Time: 72 h
Result: The half-maximal effective concentration (EC50) values against different SARS-CoV-2 variants were 95 nM (WT), 130 nM (Alpha), 277 nM (Beta), 97 nM (Delta), 86 nM (Omicron BA.1) and 158 nM (Omicron BA.5), respectively.
体内研究
(In Vivo)

Leritrelvir (RAY1216) (150-600 mg/kg/day; i.g.; 5 days) 有效延长 SARS-CoV-2 感染小鼠的生存[1]。
Compound pharmacokinetics parameters in different animal species[1]

Compound Species dose (mg/kg) Cmax (nM) Tmax (h) AUC(0-last) (nM•h) Cl (mL/min/kg) Vdss (L/kg) T1/2 (h) oral F (%)
Mouse 3.0 (IV) - - 7789 10 1.4 3.8 -
10 (PO) 1287 2.0 5698 - - 2.6 22
Leritrelvir rat 2.0 (IV) - - 4505 12.5 1.1 2.2 -
10 (PO) 916 0.9 7429 - - 4.3 33
cynomolgus macaque 1.0 (IV) - - 1157 22.5 1.0 0.9 -
5.0 (PO) 102 1.5 458 - - 14.9 8

Cmax: the maximum observed concentration of the drug collected in bodily material from subjects in a clinical study
Tmax: the time it takes to reach the maximum concentration or time to Cmax
AUC: “Area Under the Curve” and represents the total exposure of the drug experienced by the subject in a clinical study
Cl: total plasma clearance
Vdss: Steady state volume of distribution
T1/2: Half-time is the time it takes for half the drug concentration to be eliminated
oral (F%): Oral bioavailability

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

Animal Model: Female human ACE2 transgenic C57BL/6 mouse, SARS-CoV-2 infection model[1]
Dosage: 150, 300 and 600 mg/kg/day
Administration: Intragastric administration, 5 days
Result: Protected mice infected with SARS-CoV-2 by 100%, 43% and 14% at 600, 300 and 150 mg/kg, respectively. Decreased viral titres in lungs significantly compared with the infection-only group. Reduced virus induced pathology.
Animal Model: Male CD-1 mouse, male SD rat and male cynomolgus macaque[1]
Dosage: 1-10 mg/kg
Administration: PO or IV (Pharmacokinetic Analysis)
Result: Showed promising human pharmacokinetics profile.
Clinical Trial
分子量

639.71

Formula

C31H44F3N5O6
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

Leritrelvir 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:

Leritrelvir2923310-64-7RAY1216RAY 1216RAY-1216SARS-CoVSARS coronavirusantiviralSARS-CoV-2OmicronC57BL/6Vero E6Inhibitorinhibitorinhibit

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