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

Ibuzatrelvir  (Synonyms: PF-07817883)

Cat. No.: HY-156654 Purity: 99.90%
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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.

For research use only. We do not sell to patients.

Ibuzatrelvir Chemical Structure

Ibuzatrelvir Chemical Structure

CAS No. : 2755812-39-4

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1 mg USD 224 In-stock
5 mg USD 560 In-stock
10 mg USD 890 In-stock
25 mg USD 1780 In-stock
50 mg USD 2850 In-stock
100 mg USD 4560 In-stock
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Based on 1 publication(s) in Google Scholar

Ibuzatrelvir Related Antibodies

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Description

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]
In Vitro

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 Related Antibodies
In Vivo

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]

药代动力学分析[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
Molecular Weight

489.49

Formula

C21H30F3N5O5
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

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
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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.
Purity & Documentation

Purity: 99.90%

COA (257 KB) HNMR (283 KB) RP-HPLC (262 KB) LCMS (104 KB)

Handling Instructions (2659 KB)
References

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

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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