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

Ibuzatrelvir  (Synonyms: PF-07817883)

製品番号: HY-156654 純度: 99.90%
COA 取扱説明書 Technical Support

Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 main protease (Mpro and 3CLpro) inhibitor with improved metabolic stability. Ibuzatrelvir has demonstrated pan-human coronavirus antiviral activity and off-target selectivity profile in vitro and in preclinical animal studies. Ibuzatrelvir is well tolerated with a safety profile similar to placebo and prevents viral infection and transmission. Ibuzatrelvir can be used to inhibit COVID-19.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Ibuzatrelvir

Ibuzatrelvir 構造式

CAS 番号 : 2755812-39-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 603 在庫あり
Solution
10 mM * 1 mL in DMSO USD 603 在庫あり
Solid
5 mg $560 在庫あり
10 mg $890 在庫あり
25 mg $1780 在庫あり
50 mg $2850 在庫あり
100 mg $4560 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Ibuzatrelvir 関連抗体

Top Publications Citing Use of Products

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 main protease (Mpro and 3CLpro) inhibitor with improved metabolic stability. Ibuzatrelvir has demonstrated pan-human coronavirus antiviral activity and off-target selectivity profile in vitro and in preclinical animal studies. Ibuzatrelvir is well tolerated with a safety profile similar to placebo and prevents viral infection and transmission. Ibuzatrelvir can be used to inhibit COVID-19[1][2][3][4].
IC50 & Target

SARS-CoV-2 3CL protease, COVID-19[1]
体外実験

Ibuzatrelvir (0-10000 nM, 3 days) inhibits the SARS-CoV-1 Mpro and MERS Mpro activity with IC50 values of 18 nM and 930 nM, respectively. Ibuzatrelvir demostrates a potent inhibitor of the proteolytic activity of SARS-CoV-2 Mpro as well as related human coronaviruses in VeroE6, MRC-5 or Vero81 cells[4].
Ibuzatrelvir demonstrates potent SARS-CoV-2 antiviral cellular activity with EC50 and EC90 values of 34 nM and 70 nM respectively in differentiated normal human bronchial epithelial (dNHBE) cells[4].

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

Ibuzatrelvir 関連抗体
体内実験

Ibuzatrelvir (0-500 mg/kg, p.o., a single dose) inhibits virus replication in a dose-dependent manner in mouse- adapted SARS-CoV-2 animal model[4].

Pharmacokinetics of Ibuzatrelvir in Rats and Monkeys[1]

Species Route/Dose(mg/kg) CLp (mL/min/kg) Vd,ss (L/kg) T1/2 (h) CLrenal (mL/min/kg) Cmax (ng/mL) Tmax (h) AUC0 24 (ng·h/mL) Oral F (%) Fa × Fgc (%)
Rat i.v./1 34.4 (34.4, 34.4) 1.52 (1.67, 1.36) 10 (9.0, 11.2) 5.52 (3.25, 7.8) 481 (481, 481)
p.o./7.5 - 606 (665, 547) 0.29 (0.083,0.50) 793 (704, 882) 21.9 (19.5, 24.3) 41.6 (37.19, 46.59)
Monkey i.v./1 6.88 (5.46, 8.29) 0.657(0.591, 0.723) 2.77 (2.87, 2.67) 0.697 (0.0878,1.31) - - 2530 (3050, 2010) - -
p.o./10 - - - - 1510 (1650, 1360) 0.38 (0.25, 0.5) 7380 (8160, 6590) 29.2 (26.0, 32.3) 37.3 (40.8, 34.1)

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

Animal Model: mouse-adapted SARS-CoV-2 animal model[4].
Dosage: 0-500 mg/kg
Administration: p.o., a single dose
Result: Prevented weight loss and reduced the lung virus titer in mouse-adapted SARS-CoV-2 animal model
臨床実験
分子量

489.49

分子式

C21H30F3N5O5
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

COC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@H](C1)C(F)(F)F)C(N[C@H](C#N)C[C@H]2C(NCC2)=O)=O)=O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (204.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0429 mL 10.2147 mL 20.4294 mL
5 mM 0.4086 mL 2.0429 mL 4.0859 mL
10 mM 0.2043 mL 1.0215 mL 2.0429 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.90%

COA (257 KB) HNMR (284 KB) RP-HPLC (262 KB) LCMS (104 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0429 mL 10.2147 mL 20.4294 mL 51.0736 mL
5 mM 0.4086 mL 2.0429 mL 4.0859 mL 10.2147 mL
10 mM 0.2043 mL 1.0215 mL 2.0429 mL 5.1074 mL
15 mM 0.1362 mL 0.6810 mL 1.3620 mL 3.4049 mL
20 mM 0.1021 mL 0.5107 mL 1.0215 mL 2.5537 mL
25 mM 0.0817 mL 0.4086 mL 0.8172 mL 2.0429 mL
30 mM 0.0681 mL 0.3405 mL 0.6810 mL 1.7025 mL
40 mM 0.0511 mL 0.2554 mL 0.5107 mL 1.2768 mL
50 mM 0.0409 mL 0.2043 mL 0.4086 mL 1.0215 mL
60 mM 0.0340 mL 0.1702 mL 0.3405 mL 0.8512 mL
80 mM 0.0255 mL 0.1277 mL 0.2554 mL 0.6384 mL
100 mM 0.0204 mL 0.1021 mL 0.2043 mL 0.5107 mL
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Ibuzatrelvir Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
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:

Ibuzatrelvir2755812-39-4PF-07817883PF07817883PF 07817883Virus ProteaseSARS-CoVSARS coronavirusorally bioavailableSARS-CoV-2 inhibitorantiviral activityinhibit COVID-19Inhibitorinhibitorinhibit

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