Nirmatrelvir
Based on 111 publication(s) in Google Scholar
Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CLPRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.74%
- CAS. Nr.: 2628280-40-8
- Formel: C23H32F3N5O4
- Molecular Weight:499.53
-
Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Nirmatrelvir
More- N Engl J Med. 2023 Jan 5;388(1):89-91. [Abstract]
- Signal Transduct Target Ther. 2025 Jan 17;10(1):30. [Abstract]
- Nature. 2022 Jul;607(7917):119-127. [Abstract]
- Cell. 2026 Jun 25;189(13):4075-4093.e25. [Abstract]
- Nat Commun. 2025 Apr 3;16(1):2900. [Abstract]
- Nat Commun. 2023 Feb 25;14(1):1076. [Abstract]
- Nat Commun. 2023 Jul 15;14(1):4231. [Abstract]
- Nat Commun. 2023 Jul 4;14(1):3952. [Abstract]
- Sci Immunol. 2023 Apr 14;8(82):eadf0348. [Abstract]
- Acta Pharm Sin B. 2024 Sep;14(9):4028-4044. [Abstract]
- Phytomedicine. 2025 Jun 17:145:156989. [Abstract]
- J Hazard Mater. 2024 Jun 4:474:134823. [Abstract]
- J Transl Med. 2022 Nov 26;20(1):549. [Abstract]
- Proc Natl Acad Sci U S A. 2026 Jan 13;123(2):e2530209123. [Abstract]
- Proc Natl Acad Sci U S A. 2024 Sep 10;121(37):e2404175121. [Abstract]
- Int J Biol Macromol. 2024 Sep 4:135352. [Abstract]
- Int J Biol Macromol. 2024 Jun 27:133451. [Abstract]
- Free Radic Biol Med. 2024 Aug 1:220:167-178. [Abstract]
- Cell Rep. 2024 Nov 5;43(11):114929. [Abstract]
- Anal Chem. 2026 Jun 23. [Abstract]
- J Med Chem. 2026 Jan 22;69(2):1530-1551. [Abstract]
- J Med Chem. 2024 Oct 24;67(20):18478-18490. [Abstract]
- J Med Chem. 2024 Sep 12;67(17):14986-15011. [Abstract]
- J Med Chem. 2024 Aug 8;67(15):12760-12783. [Abstract]
- J Med Chem. 2023 Oct 12;66(19):13516-13529. [Abstract]
- Eur J Med Chem. 2022 Mar 5:231:114130. [Abstract]
- Cell Biosci. 2024 Sep 6;14(1):115. [Abstract]
- Commun Biol. 2025 Jul 17;8(1):1061. [Abstract]
- Commun Biol. 2022 Sep 16;5(1):976. [Abstract]
- Int J Mol Sci. 2023 Mar 23;24(7):6062. [Abstract]
- mBio. 2023 Oct 31;14(5):e0158723. [Abstract]
- J Enzyme Inhib Med Chem. 2023 Dec;38(1):2251721. [Abstract]
- ACS Omega. 2026 Jan 14;11(3):4541-4550. [Abstract]
- ACS Omega. 2025 Aug 27;10(36):41608-41619. [Abstract]
- Molecules. 2025 Jan 17;30(2):387. [Abstract]
- Biomol Ther (Seoul). 2024 Jul 1;32(4):481-491. [Abstract]
- PNAS Nexus. 2025 Jan 7;4(1):pgae578. [Abstract]
- RSC Med Chem. 2024 Sep 27;15(12):4193-4205. [Abstract]
- Int J Infect Dis. 2024 Jun 27:107134. [Abstract]
- iScience. 2024 Aug 17;27(9):110729. [Abstract]
- iScience. 2023 Oct 4;26(11):108147. [Abstract]
- iScience. 2022 Nov 18;25(11):105365. [Abstract]
- Antiviral Res. 2026 Jul:251:106445. [Abstract]
- Antiviral Res. 2025 Jun 10:106212. [Abstract]
- Antiviral Res. 2024 Jan:221:105766. [Abstract]
- Antiviral Res. 2023 Aug:216:105671. [Abstract]
- Mol Hum Reprod. 2026 Feb 26:gaag015. [Abstract]
- Antimicrob Agents Chemother. 2025 Apr 2;69(4):e0155624. [Abstract]
- J Antimicrob Chemother. 2025 Oct 3;80(10):2807-2813. [Abstract]
- J Biol Chem. 2024 Aug 9:107675. [Abstract]
- J Virol. 2024 Feb 20;98(2):e0121623. [Abstract]
- J Virol. 2023 Aug 31;97(8):e0059723. [Abstract]
- J Biol Chem. 2023 Jul;299(7):104886. [Abstract]
- J Virol. 2022 Apr 27;96(8):e0201321. [Abstract]
- ACS Pharmacol Transl Sci. 2026 Jan 28.
- Microbe. 2025 Oct 14.
- Pathogens. 2026 Mar 18;15(3):324. [Abstract]
- Viruses. 2025 Dec 27.
- Viruses. 2025 Mar 12;17(3):402. [Abstract]
- Viruses. 2024 Apr 29, 16(5), 708.
- Viruses. 2023 Jul 19;15(7):1577. [Abstract]
- Viruses. 2023 Mar 30;15(4):891. [Abstract]
- Viruses. 2022 Sep 12;14(9):2017. [Abstract]
- Viruses. 2022 Jun 23;14(7):1369. [Abstract]
- J Med Virol. 2026 Feb;98(2):e70855. [Abstract]
- Drug Metab Dispos. 2025 Sep 8;53(10):100158. [Abstract]
- Npj Viruses. 2024 Jan 24;2(1):4. [Abstract]
- J Pharm Biomed Anal. 2024 Aug 1:245:116162. [Abstract]
- SLAS Discov. 2026 Aug:41:100311. [Abstract]
- SLAS Discov. 2024 May 16:100160. [Abstract]
- Adv Biol (Weinh). 2024 Aug 9:e2300511. [Abstract]
- Int J Anal Chem. 2025 Nov 17:2025:6625833. [Abstract]
- PLoS One. 2023 Sep 14;18(9):e0291537. [Abstract]
- Toxicol In Vitro. 2024 May 19:105848. [Abstract]
- Vet Sci. 2023 Aug 9;10(8):513. [Abstract]
- Virology. 2026 Jul:620:110915. [Abstract]
- Biochem Biophys Res Commun. 2026 Aug 27:828:153866. [Abstract]
- Biochem Biophys Res Commun. 2023 Nov 19:682:138-140. [Abstract]
- Bioorg Med Chem Lett. 2022 Apr 15;62:128629. [Abstract]
- bioRxiv. 2026 May 26:2026.05.26.725122. [Abstract]
- bioRxiv. 2026 May 12.
- bioRxiv. 2025 Dec 19.
- bioRxiv. 2025 Nov 17.
- Res Sq. 2025 Jul 29.
- bioRxiv. 2025 May 30:2025.05.28.656516. [Abstract]
- Res Sq. 2025 Apr 20.
- Patent. US20250123269A1.
- bioRxiv. 2025 March 11.
- bioRxiv. 2025 January 18.
- Res Sq. 2024 Nov 21:rs.3.rs-5454588. [Abstract]
- bioRxiv. 2024 Aug 29:2024.08.08.606661. [Abstract]
- Heliyon. 2024 Jul 20;10(15):e34820. [Abstract]
- medRxiv. 2024 Jun 18:2024.06.14.24308523. [Abstract]
- bioRxiv. 2024 Jun 3:2024.06.02.596989. [Abstract]
- bioRxiv. 2024 Apr 17.
- Heliyon. 2024 Jan 10;10(2):e24333. [Abstract]
- Preprints. 2024 Jan 3.
- SSRN. 2024 Jan 26.
- bioRxiv. 2023 Nov 27.
- bioRxiv. 2024 Feb 9:2023.11.20.567873. [Abstract]
- bioRxiv. 2023 Oct 21.
- bioRxiv. 2023 Aug 23.
- bioRxiv. 2023 Jun 28.
- bioRxiv. 2023 Jun 28:2023.06.27.546784. [Abstract]
- Preprints. 2023 Jun 1.
- bioRxiv. 2023 Feb 27:2023.02.25.530000. [Abstract]
- bioRxiv. 2023 Jun 25:2023.03.23.533961. [Abstract]
- Preprints. 2022, 2022060272.
- Preprints. 2022, 2022050381.
- Res Sq. 2022 Feb 11:rs.3.rs-1318037. [Abstract]
- Res Sq. 2022 Feb 24:rs.3.rs-1375091. [Abstract]
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In Vivo Efficacy Study
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Histological Imaging/Staining
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Histological Imaging/Staining
Biologische Aktivität
IC50: 3CLPRO[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | CC50 |
>100 μM
Compound: Nirmatrelvir
|
Cytotoxicity against human Caco-2 cells assessed as reduction in cell viability
Cytotoxicity against human Caco-2 cells assessed as reduction in cell viability
|
[PMID: 38432056] |
| Calu-3 | CC50 |
>100 μM
Compound: Nirmatrelvir
|
Cytotoxicity against human Calu-3 cells assessed as reduction in cell viability
Cytotoxicity against human Calu-3 cells assessed as reduction in cell viability
|
[PMID: 38432056] |
| CCRF-CEM | CC50 |
>100 μM
Compound: Nirmatrelvir
|
Cytotoxicity against human CEM cells assessed as reduction in cell viability
Cytotoxicity against human CEM cells assessed as reduction in cell viability
|
[PMID: 38432056] |
| Epithelial cell | EC50 |
25.3 nM
Compound: PF-07321332
|
Antiviral activity against SARS-CoV-2 infected in human Primary bronchial epithelial cell assessed as inhibition of viral growth
Antiviral activity against SARS-CoV-2 infected in human Primary bronchial epithelial cell assessed as inhibition of viral growth
|
[PMID: 38335279] |
| HCT-8 | CC50 |
>30 μM
Compound: PF-07321332
|
Cytotoxicity against human HCT-8 cells incubated for 120 hrs by Cell-Titer Glo assay
Cytotoxicity against human HCT-8 cells incubated for 120 hrs by Cell-Titer Glo assay
|
[PMID: 38335279] |
| HEK-293T | CC50 |
>50000 nM
Compound: PF-07321332
|
Cytotoxicity against HEK293T cells transfected with ACE2 and TMPRSS2 assessed as reduction in cell viability
Cytotoxicity against HEK293T cells transfected with ACE2 and TMPRSS2 assessed as reduction in cell viability
|
[PMID: 36229406] |
| HeLa | CC50 |
>40 μM
Compound: PF-07321332
|
Cytotoxicity against human HeLa cells expressing ACE2 incubated for 120 hrs by Cell-Titer Glo assay
Cytotoxicity against human HeLa cells expressing ACE2 incubated for 120 hrs by Cell-Titer Glo assay
|
[PMID: 38335279] |
| Huh-7 | CC50 |
>100 μM
Compound: Nirmatrelvir
|
Cytotoxicity against human Huh-7 cells overexpressing human ACE2 assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human Huh-7 cells overexpressing human ACE2 assessed as reduction in cell viability incubated for 24 hrs by MTT assay
|
[PMID: 36549112] |
| Huh-7 | CC50 |
>100 μM
Compound: Nirmatrelvir
|
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability
|
[PMID: 38432056] |
| Huh-7 | CC50 |
>50000 nM
Compound: 4
|
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 7 days by Celltiter -Glo assay
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 7 days by Celltiter -Glo assay
|
[PMID: 38518735] |
| MRC5 | EC50 |
0.212 μM
Compound: Nirmatrelvir
|
Antiviral activity against against Human coronavirus 229E infected in human MRC5 cells assessed as reduction in cell viability measured after 4 days by CellTiter-Glo luminescence assay
Antiviral activity against against Human coronavirus 229E infected in human MRC5 cells assessed as reduction in cell viability measured after 4 days by CellTiter-Glo luminescence assay
|
[PMID: 35971455] |
| MRC5 | CC50 |
>30 μM
Compound: PF-07321332
|
Cytotoxicity against human MRC5 cells incubated for 120 hrs by Cell-Titer Glo assay
Cytotoxicity against human MRC5 cells incubated for 120 hrs by Cell-Titer Glo assay
|
[PMID: 38335279] |
| MRC5 | CC50 |
>50000 nM
Compound: 4
|
Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 7 days by Celltiter -Glo assay
Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 7 days by Celltiter -Glo assay
|
[PMID: 38518735] |
| PBMC | CC50 |
>100 μM
Compound: Nirmatrelvir
|
Cytotoxicity against human PBMC cells assessed as reduction in cell viability
Cytotoxicity against human PBMC cells assessed as reduction in cell viability
|
[PMID: 38432056] |
| Vero | CC50 |
>25 μM
Compound: Nirmatrevir
|
Cytotoxicity against african green monkey Vero cells
Cytotoxicity against african green monkey Vero cells
|
[PMID: 36870624] |
| Vero | CC50 |
>100 μM
Compound: Nirmatrelvir
|
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability
|
[PMID: 38432056] |
| Vero C1008 | EC50 |
75 nM
Compound: 13
|
Antiviral activity against SARS Cov-2 infected in Vero E6 cells expressing hACE2 assessed as virus induced cytopathic effect incubated for 3 day by Cell Titer-Glo assay
Antiviral activity against SARS Cov-2 infected in Vero E6 cells expressing hACE2 assessed as virus induced cytopathic effect incubated for 3 day by Cell Titer-Glo assay
|
[PMID: 35291756] |
| Vero C1008 | CC50 |
>50000 nM
Compound: PF-07321332
|
Cytotoxicity against African green monkey Vero E6 cells transfected with TMPRSS2 assessed as reduction in cell viability
Cytotoxicity against African green monkey Vero E6 cells transfected with TMPRSS2 assessed as reduction in cell viability
|
[PMID: 36229406] |
| Vero C1008 | CC50 |
>100 μM
Compound: Nirmatrelvir
|
Cytotoxicity against african green monkey Vero E6 cells assessed as reduction in cell viability after 26 hrs by MTS assay
Cytotoxicity against african green monkey Vero E6 cells assessed as reduction in cell viability after 26 hrs by MTS assay
|
[PMID: 36475694] |
| Vero C1008 | EC50 |
0.075 μM
Compound: Nirmatrelvir
|
Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as reduction in virus induced cytopathic effect incubated for 3 days
Antiviral activity against SARS-CoV-2 infected in Vero E6 cells assessed as reduction in virus induced cytopathic effect incubated for 3 days
|
[PMID: 36475694] |
| Vero C1008 | EC50 |
21.7 nM
Compound: PF-07321332
|
Antiviral activity against SARS-CoV-2 variant Omicron BA.2 infected in African green monkey Vero E6 cells assessed as reduction in virus-induced cytopathic effect
Antiviral activity against SARS-CoV-2 variant Omicron BA.2 infected in African green monkey Vero E6 cells assessed as reduction in virus-induced cytopathic effect
|
[PMID: 37229831] |
| Vero C1008 | EC50 |
0.074 μM
Compound: 1; PF-07321332
|
Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in viral growth incubated for 24 hrs by fluorescence based analysis
Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in viral growth incubated for 24 hrs by fluorescence based analysis
|
[PMID: 37244162] |
| Vero C1008 | CC50 |
>500 μM
Compound: Nirmatrelvir
|
Cytotoxicity against African green monkey Vero E6 cells incubated for 48 hrs by Luminescent cell viability assay
Cytotoxicity against African green monkey Vero E6 cells incubated for 48 hrs by Luminescent cell viability assay
|
[PMID: 37253309] |
| Vero C1008 | CC50 |
>500 μM
Compound: 1
|
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay
|
[PMID: 37594952] |
| Vero C1008 | EC50 |
0.729 μM
Compound: 1
|
Antiviral activity against SARS-CoV-2 B1.617.2 (Delta) infected in african green monkey Vero E6 cells assessed as reduction in viral replication incubated for 24 hrs by qRT-PCR analysis
Antiviral activity against SARS-CoV-2 B1.617.2 (Delta) infected in african green monkey Vero E6 cells assessed as reduction in viral replication incubated for 24 hrs by qRT-PCR analysis
|
[PMID: 37594952] |
| Vero C1008 | CC50 |
>100 μM
Compound: 1
|
Cytotoxicity against African green monkey Vero E6 cells incubated for 3 days by WST-8 assay
Cytotoxicity against African green monkey Vero E6 cells incubated for 3 days by WST-8 assay
|
[PMID: 37756225] |
| Vero C1008 | CC50 |
>100 μM
Compound: 1
|
Cytotoxicity in African green monkey Vero E6 cells measured after 25 days by Neutral red release assay
Cytotoxicity in African green monkey Vero E6 cells measured after 25 days by Neutral red release assay
|
[PMID: 37992202] |
3CLPRO is responsible for cleaving polyproteins 1a and 1ab of SARS-CoV-2.1. Without the activity of the SARS-CoV-2 3CLPRO, nonstructural proteins (including proteases) cannot be released to perform their functions, inhibiting viral replication[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS. Nr. 2628280-40-8
-
Appearance Solid
-
Molecular Weight 499.53
-
Formel C23H32F3N5O4
-
Color White to off-white
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SMILES
O=C(NCC1)[C@@H]1C[C@@H](C#N)NC([C@@H]2[C@]3([H])[C@@](CN2C([C@H](C(C)(C)C)NC(C(F)(F)F)=O)=O)([H])C3(C)C)=O
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Synonyms
PF-07321332
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (111)
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Journal Impact Factor
-
Most Recent
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N Engl J Med
2023 Jan 5;388(1):89-91. PMID: 36476720
Nirmatrelvir purchased from MedChemExpress. Usage Cited in: N Engl J Med. 2023 Jan 5;388(1):89-91. [Abstract]
Remdesivir, Molnupiravir, and Nirmatrelvir are efficacious against both BQ.1.1 and XBB in vitro.
Nirmatrelvir purchased from MedChemExpress. Usage Cited in: N Engl J Med. 2023 Jan 5;388(1):89-91. [Abstract]
Representative echocardiographic images (M-mode) from sham, TAC and Tipifarnib (10 mg/kg body weight/three times a week, IP injection) treated TAC mouse heart at 8 weeks.
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Signal Transduct Target Ther
Real-world effectiveness and safety of oral azvudine versus nirmatrelvir‒ritonavir (Paxlovid) in hospitalized patients with COVID-19: a multicenter, retrospective, cohort study. [Abstract]2025 Jan 17;10(1):30. PMID: 39819859 -
Nature
2022 Jul;607(7917):119-127. PMID: 35576972
Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Nature. 2022 Jul;607(7917):119-127. [Abstract]
Syrian hamsters were intranasally inoculated with 103 PFU of BA.2 (NCD1288). One day after infection, hamsters were treated with: 500 mg kg−1 molnupiravir, 1,000 mg kg−1 nirmatrelvir or 60 mg kg−1 S-217622 orally twice daily for 3 days. Methylcellulose served as a control for oral treatment. Eight hamsters per group were euthanized at 4 dpi for virus titration. Viral titres in the nasal turbinates and lungs were determined by plaque assay.
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Cell
Virological characteristics of SARS-CoV-2-related coronaviruses dynamically circulating in Southeast Asia. [Abstract]2026 Jun 25;189(13):4075-4093.e25. PMID: 42097139 -
Nat Commun
2025 Apr 3;16(1):2900. PMID: 40180914
Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 3;16(1):2900. [Abstract]
Mice were treated at 6 h, 24 h and 48 h with euthanasia performed at 72 h post-infection. WT 7-9 week-old mice were infected with SARS-CoV-2 P21 and treated with either vehicle, PLT (Paxlovid-like treatment: 56 mg/kg Nirmatrelvir, 19 mg/kg Ritonavir), or WEHI-P8 (100 mg/kg or 150 mg/kg). Three days post-infection, mice were monitored for d viral load and percentage change in body weight compared to initial body weight.
Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 3;16(1):2900. [Abstract]
H&E staining showed that mice in the PLT treatment group (Paxlovid-like treatment: 56 mg/kg Nirmatrelvir, 19 mg/kg Ritonavir) exhibited mild to moderate multifocal inflammation, mainly confined to the peribronchial and perivascular areas of the lungs, with occasional alveolar collapse and mild hemorrhages.
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Nat Commun
Identification of SARS-CoV-2 Mpro inhibitors containing P1' 4-fluorobenzothiazole moiety highly active against SARS-CoV-2. [Abstract]2023 Feb 25;14(1):1076. PMID: 36841831 -
Nat Commun
2023 Jul 15;14(1):4231. PMID: 37454219 -
Nat Commun
2023 Jul 4;14(1):3952. PMID: 37402789 -
Sci Immunol
Inhibition of the mitochondrial pyruvate carrier simultaneously mitigates hyperinflammation and hyperglycemia in COVID-19. [Abstract]2023 Apr 14;8(82):eadf0348. PMID: 36821695
Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Sci Immunol. 2023 Apr 14;8(82):eadf0348. [Abstract]
DIO mice were infected with SARS-CoV-2 MA10 virus and treated with vehicle, Nirmatrelvir, or Nirmatrelvir plus MSDC. Host mortality was monitored and survival rate is shown.
Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Sci Immunol. 2023 Apr 14;8(82):eadf0348. [Abstract]
DIO mice were infected with SARS-CoV-2 MA10 virus and treated with vehicle, Nirmatrelvir, or Nirmatrelvir plus MSDC. H&E staining of lung section (n = 5) and quantification of pathological lesions at 21 d.p.i. Scale bar, 200 μm. HM, hyaline membranes.
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Acta Pharm Sin B
2024 Sep;14(9):4028-4044. PMID: 39309487 -
Phytomedicine
Dihydrotanshinone I targets the spike N-terminal domain to inhibit SARS-CoV-2 entry and spike-induced inflammation. [Abstract]2025 Jun 17:145:156989. PMID: 40570554 -
J Hazard Mater
Polystyrene nanoplastics induce cardiotoxicity by upregulating HIPK2 and activating the P53 and TGF-β1/Smad3 pathways. [Abstract]2024 Jun 4:474:134823. PMID: 38852254 -
J Transl Med
Paxlovid accelerates cartilage degeneration and senescence through activating endoplasmic reticulum stress and interfering redox homeostasis. [Abstract]2022 Nov 26;20(1):549. PMID: 36435786 -
Proc Natl Acad Sci U S A
Combination antiviral and anti-inflammatory therapy mitigates persistent neurological deficits in mice post SARS-CoV-2 infection. [Abstract]2026 Jan 13;123(2):e2530209123. PMID: 41499397 -
Proc Natl Acad Sci U S A
Structural and virologic mechanism of the emergence of resistance to Mpro inhibitors in SARS-CoV-2. [Abstract]2024 Sep 10;121(37):e2404175121. PMID: 39236245 -
Int J Biol Macromol
Identification of novel broad-spectrum antiviral drugs targeting the N-terminal domain of the FIPV nucleocapsid protein. [Abstract]2024 Sep 4:135352. PMID: 39242012 -
Int J Biol Macromol
2024 Jun 27:133451. PMID: 38944088 -
Free Radic Biol Med
Dopamine and its precursor levodopa inactivate SARS-CoV-2 main protease by forming a quinoprotein. [Abstract]2024 Aug 1:220:167-178. PMID: 38718952 -
Cell Rep
An oral non-covalent non-peptidic inhibitor of SARS-CoV-2 Mpro ameliorates viral replication and pathogenesis in vivo. [Abstract]2024 Nov 5;43(11):114929. PMID: 39504242 -
Anal Chem
Decoding Enzyme-Inhibitor Kinetic Mechanisms by Isothermal Titration Calorimetry: The Case of SARS-CoV-2 3CLpro. [Abstract]2026 Jun 23. PMID: 42334227 -
J Med Chem
Discovery of Coronavirus Main Protease Inhibitors with Enhanced Brain Exposure and Potent Oral Efficacy in SARS-CoV-2 and MERS Infection Models. [Abstract]2026 Jan 22;69(2):1530-1551. PMID: 41490206 -
J Med Chem
Effects of SARS-CoV-2 Main Protease Mutations at Positions L50, E166, and L167 Rendering Resistance to Covalent and Noncovalent Inhibitors. [Abstract]2024 Oct 24;67(20):18478-18490. PMID: 39370853 -
J Med Chem
Nonpeptidic Irreversible Inhibitors of SARS-CoV-2 Main Protease with Potent Antiviral Activity. [Abstract]2024 Sep 12;67(17):14986-15011. PMID: 39146284 -
J Med Chem
Discovery of Novel Nonpeptidic and Noncovalent Small Molecule 3CLpro Inhibitors as anti-SARS-CoV-2 Drug Candidate. [Abstract]2024 Aug 8;67(15):12760-12783. PMID: 39072488 -
J Med Chem
Structure-Activity Relationship Studies of SARS-CoV-2 Main Protease Inhibitors Containing 4-Fluorobenzothiazole-2-carbonyl Moieties. [Abstract]2023 Oct 12;66(19):13516-13529. PMID: 37756225 -
Eur J Med Chem
In silico screening-based discovery of novel covalent inhibitors of the SARS-CoV-2 3CL protease. [Abstract]2022 Mar 5:231:114130. PMID: 35114541 -
Cell Biosci
Targeting stress induction of GRP78 by cardiac glycoside oleandrin dually suppresses cancer and COVID-19. [Abstract]2024 Sep 6;14(1):115. PMID: 39238058 -
Commun Biol
Characterization of an unusual SARS-CoV-2 main protease natural variant exhibiting resistance to nirmatrelvir and ensitrelvir. [Abstract]2025 Jul 17;8(1):1061. PMID: 40676153 -
Commun Biol
Autoprocessing and oxyanion loop reorganization upon GC373 and nirmatrelvir binding of monomeric SARS-CoV-2 main protease catalytic domain. [Abstract]2022 Sep 16;5(1):976. PMID: 36114420 -
Int J Mol Sci
Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir. [Abstract]2023 Mar 23;24(7):6062. PMID: 37047038 -
mBio
Pyronaridine tetraphosphate is an efficacious antiviral and anti-inflammatory active against multiple highly pathogenic coronaviruses. [Abstract]2023 Oct 31;14(5):e0158723. PMID: 37581442 -
J Enzyme Inhib Med Chem
The hope and hype of ellagic acid and urolithins as ligands of SARS-CoV-2 Nsp5 and inhibitors of viral replication. [Abstract]2023 Dec;38(1):2251721. PMID: 37638806 -
ACS Omega
Impact of Single Halogen Atom Substitutions on Antiviral Profile of Inhibitors Targeting SARS-CoV‑2 Main Protease. [Abstract]2026 Jan 14;11(3):4541-4550. PMID: 41626465 -
ACS Omega
SARS-CoV‑2 Main Protease Inhibitors Containing 5‑Substituted Benzothiazole-2-carbonyl Moieties at the P1' Site and Their Derivatives. [Abstract]2025 Aug 27;10(36):41608-41619. PMID: 40978346 -
Molecules
Antiviral Activity and Underlying Mechanism of Moslae herba Aqueous Extract for Treating SARS-CoV-2. [Abstract]2025 Jan 17;30(2):387. PMID: 39860255 -
Biomol Ther (Seoul)
Analysis of SARS-CoV-2 Mutations after Nirmatrelvir Treatment in a Lung Cancer Xenograft Mouse Model. [Abstract]2024 Jul 1;32(4):481-491. PMID: 38835145 -
PNAS Nexus
An orally available P1'-5-fluorinated Mpro inhibitor blocks SARS-CoV-2 replication without booster and exhibits high genetic barrier. [Abstract]2025 Jan 7;4(1):pgae578. PMID: 39831159 -
RSC Med Chem
Discovery of a nasal spray steroid, tixocortol, as an inhibitor of SARS-CoV-2 main protease and viral replication. [Abstract]2024 Sep 27;15(12):4193-4205. PMID: 39371432 -
Int J Infect Dis
Antiviral susceptibility of SARS-CoV-2 and influenza viruses from 3 co-infected pediatric patients. [Abstract]2024 Jun 27:107134. PMID: 38944411 -
iScience
Drug susceptibility and the potential for drug-resistant SARS-CoV-2 emergence in immunocompromised animals. [Abstract]2024 Aug 17;27(9):110729. PMID: 39280602 -
iScience
2023 Oct 4;26(11):108147. PMID: 37876803 -
iScience
2022 Nov 18;25(11):105365. PMID: 36338434 -
Antiviral Res
2026 Jul:251:106445. PMID: 42162876 -
Antiviral Res
2025 Jun 10:106212. PMID: 40505777 -
Antiviral Res
Broad-spectrum antiviral activity of two structurally analogous CYP3A inhibitors against pathogenic human coronaviruses in vitro. [Abstract]2024 Jan:221:105766. PMID: 38042417 -
Antiviral Res
Assessment of the frequency of SARS-CoV-2 Omicron variant escape from RNA-dependent RNA polymerase inhibitors and 3C-like protease inhibitors. [Abstract]2023 Aug:216:105671. PMID: 37451629 -
Mol Hum Reprod
SARS-CoV-2 infects human primary cytotrophoblasts mainly through a non-canonical entry route. [Abstract]2026 Feb 26:gaag015. PMID: 41755626 -
Antimicrob Agents Chemother
Potent antiviral activity of simnotrelvir against key epidemic SARS-CoV-2 variants with a high resistance barrier. [Abstract]2025 Apr 2;69(4):e0155624. PMID: 40062859 -
J Antimicrob Chemother
Placental transfer of medications to treat COVID-19, molnupiravir, favipiravir and nirmatrelvir/ritonavir, in the ex vivo human cotyledon model. [Abstract]2025 Oct 3;80(10):2807-2813. PMID: 40888812 -
J Biol Chem
2024 Aug 9:107675. PMID: 39128719 -
J Virol
2024 Feb 20;98(2):e0121623. PMID: 38236006 -
J Virol
2023 Aug 31;97(8):e0059723. PMID: 37578235 -
J Biol Chem
Contribution of the catalytic dyad of SARS-CoV-2 main protease to binding covalent and noncovalent inhibitors. [Abstract]2023 Jul;299(7):104886. PMID: 37271339 -
J Virol
Structural Basis of the Main Proteases of Coronavirus Bound to Drug Candidate PF-07321332. [Abstract]2022 Apr 27;96(8):e0201321. PMID: 35389231 -
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Pathogens
Antiviral Activity of Pyrazolopyrimidine and Triazolopyrimidine Derivatives Against SARS-CoV-2 In Vitro: Identifying PZP25 as a Promising Scaffold. [Abstract]2026 Mar 18;15(3):324. PMID: 41901777 -
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Viruses
Biochemical Screening of Phytochemicals and Identification of Scopoletin as a Potential Inhibitor of SARS-CoV-2 Mpro, Revealing Its Biophysical Impact on Structural Stability. [Abstract]2025 Mar 12;17(3):402. PMID: 40143329 -
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Viruses
Synergistic Activity of Remdesivir-Nirmatrelvir Combination on a SARS-CoV-2 In Vitro Model and a Case Report. [Abstract]2023 Jul 19;15(7):1577. PMID: 37515263 -
Viruses
Discovery of Potential Inhibitors of SARS-CoV-2 Main Protease by a Transfer Learning Method. [Abstract]2023 Mar 30;15(4):891. PMID: 37112871 -
Viruses
Molecular Analyses of Clinical Isolates and Recombinant SARS-CoV-2 Carrying B.1 and B.1.617.2 Spike Mutations Suggest a Potential Role of Non-Spike Mutations in Infection Kinetics. [Abstract]2022 Sep 12;14(9):2017. PMID: 36146823 -
Viruses
A Newly Engineered A549 Cell Line Expressing ACE2 and TMPRSS2 Is Highly Permissive to SARS-CoV-2, Including the Delta and Omicron Variants. [Abstract]2022 Jun 23;14(7):1369. PMID: 35891350 -
J Med Virol
SARS-CoV-2 Main Protease Activates ERK1/2 Signaling to Facilitate MEG2-STAT3-Mediated Suppression of ACE2. [Abstract]2026 Feb;98(2):e70855. PMID: 41728757 -
Drug Metab Dispos
Mechanistic insights into human carboxylesterase 2 (CES2) inhibition by the CES1 prodrug substrate remdesivir. [Abstract]2025 Sep 8;53(10):100158. PMID: 41061301 -
Npj Viruses
The anti-COVID-19 drug Paxlovid crosses biological barriers of the placenta and brain in rats. [Abstract]2024 Jan 24;2(1):4. PMID: 40295802 -
J Pharm Biomed Anal
Pharmacokinetic analysis of antiviral drug ritonavir across the blood-brain barrier and its interaction with Scutellaria baicalensis using multisite microdialysis in rats. [Abstract]2024 Aug 1:245:116162. PMID: 38678857 -
SLAS Discov
Repurposing drug screen for the identification of helicase inhibitors from viruses of pandemic concern. [Abstract]2026 Aug:41:100311. PMID: 42067193 -
SLAS Discov
2024 May 16:100160. PMID: 38761981 -
Adv Biol (Weinh)
Predicting Clinical Outcomes of SARS-CoV-2 Drug Efficacy with a High-Throughput Human Airway Microphysiological System. [Abstract]2024 Aug 9:e2300511. PMID: 39123296 -
Int J Anal Chem
2025 Nov 17:2025:6625833. PMID: 41321979 -
PLoS One
Animal efficacy study of a plant extract complex (BEN815) as a potential treatment for COVID-19. [Abstract]2023 Sep 14;18(9):e0291537. PMID: 37708114 -
Toxicol In Vitro
Nirmatrelvir has detrimental effects on sperm function by altering the PI3K/PDK1/AKT signaling pathway. [Abstract]2024 May 19:105848. PMID: 38772495 -
Vet Sci
Comparative Evaluation of GS-441524, Teriflunomide, Ruxolitinib, Molnupiravir, Ritonavir, and Nirmatrelvir for In Vitro Antiviral Activity against Feline Infectious Peritonitis Virus. [Abstract]2023 Aug 9;10(8):513. PMID: 37624300
Nirmatrelvir purchased from MedChemExpress. Usage Cited in: Vet Sci. 2023 Aug 9;10(8):513. [Abstract]
The CC50, EC50, and SI for six compounds against FIPV. The half-maximal cytotoxic concentration (CC50) values are from four measurements of diluted drugs using MTT assay, in CRFK cells treated with drugs for 48 h. The half-maximal effective concentration (EC50) values are from six measurements of diluted drugs against FIPV replication in CRFK cells for 48 h. Based on the SI value (mean CC50)/(mean EC50), GS-441524 was found highly selective (SI 165.5) against FIPV among the drugs tested and showed high efficacy (EC50 1.6 µM) against FIPV with a less deleterious effect (CC50 260.0 µM) on the cells. Nirmatrelvir also showed promising efficacy (EC50 2.5 µM) and selectivity (SI 113.7) against FIPV. Ritonavir showed the highest toxicity level in the cells (CC50 39.9).
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Virology
SARS-CoV-2 variant-specific enhancement of dendritic heparan sulfate mimetic antiviral activities. [Abstract]2026 Jul:620:110915. PMID: 42025022 -
Biochem Biophys Res Commun
Targeting the conserved RNA-dependent RNA polymerase with antisense oligonucleotides suppresses SARS-CoV-2 variants. [Abstract]2026 Aug 27:828:153866. PMID: 42259197 -
Biochem Biophys Res Commun
Paxlovid mouth likely is mediated by activation of the TAS2R1 bitter receptor by nirmatrelvir. [Abstract]2023 Nov 19:682:138-140. PMID: 37806252 -
Bioorg Med Chem Lett
2022 Apr 15;62:128629. PMID: 35182772 -
bioRxiv
Transgenic human dipeptidyl peptidase-4 Syrian hamsters support MERS coronavirus infection and contact transmission. [Abstract]2026 May 26:2026.05.26.725122. PMID: 42244650 -
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bioRxiv
A non-spike nucleocapsid R204P mutation in SARS-CoV-2 Omicron XEC enhances inflammation and pathogenicity. [Abstract]2025 May 30:2025.05.28.656516. PMID: 40502047 -
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Res Sq
An orally available Mpro/TMPRSS2 bispecific inhibitor with potent anti-coronavirus efficacy in vivo. [Abstract]2024 Nov 21:rs.3.rs-5454588. PMID: 39606435 -
bioRxiv
2024 Aug 29:2024.08.08.606661. PMID: 39149230 -
Heliyon
The anti-COVID-19 drug nirmatrelvir crosses the blood‒brain barrier and exhibits herb-drug pharmacokinetic interactions with Scutellaria baicalensis formulations. [Abstract]2024 Jul 20;10(15):e34820. PMID: 39170551 -
medRxiv
Emergence of transmissible SARS-CoV-2 variants with decreased sensitivity to antivirals in immunocompromised patients with persistent infections. [Abstract]2024 Jun 18:2024.06.14.24308523. PMID: 38946967 -
bioRxiv
2024 Jun 3:2024.06.02.596989. PMID: 38895239 -
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Heliyon
Pharmacokinetic analysis of placental transfer of ritonavir as a component of paxlovid using microdialysis in pregnant rats. [Abstract]2024 Jan 10;10(2):e24333. PMID: 38293424 -
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bioRxiv
Distinct evolution of SARS-CoV-2 Omicron XBB and BA.2.86/JN.1 lineages combining increased fitness and antibody evasion. [Abstract]2024 Feb 9:2023.11.20.567873. PMID: 38045308 -
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bioRxiv
Efficacy of the oral nucleoside prodrug GS-5245 (Obeldesivir) against SARS-CoV-2 and coronaviruses with pandemic potential. [Abstract]2023 Jun 28:2023.06.27.546784. PMID: 37425890 -
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bioRxiv
2023 Feb 27:2023.02.25.530000. PMID: 36909573 -
bioRxiv
Adverse outcomes in SARS-CoV-2 infected pregnant mice are gestational age-dependent and resolve with antiviral treatment. [Abstract]2023 Jun 25:2023.03.23.533961. PMID: 36993658 -
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Res Sq
Covalent narlaprevir- and boceprevir-derived hybrid inhibitors of SARS-CoV-2 main protease: room-temperature X-ray and neutron crystallography, binding thermodynamics, and antiviral activity. [Abstract]2022 Feb 11:rs.3.rs-1318037. PMID: 35169792 -
Res Sq
2022 Feb 24:rs.3.rs-1375091. PMID: 35233565
Lösungsmittel & Löslichkeit
DMSO : 140 mg/mL (280.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 50 mg/mL (100.09 mM; Need ultrasonic)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
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. 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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.0019 mL | 10.0094 mL | 20.0188 mL | 50.0470 mL |
| 5 mM | 0.4004 mL | 2.0019 mL | 4.0038 mL | 10.0094 mL | |
| 10 mM | 0.2002 mL | 1.0009 mL | 2.0019 mL | 5.0047 mL | |
| 15 mM | 0.1335 mL | 0.6673 mL | 1.3346 mL | 3.3365 mL | |
| 20 mM | 0.1001 mL | 0.5005 mL | 1.0009 mL | 2.5024 mL | |
| 25 mM | 0.0801 mL | 0.4004 mL | 0.8008 mL | 2.0019 mL | |
| 30 mM | 0.0667 mL | 0.3336 mL | 0.6673 mL | 1.6682 mL | |
| 40 mM | 0.0500 mL | 0.2502 mL | 0.5005 mL | 1.2512 mL | |
| 50 mM | 0.0400 mL | 0.2002 mL | 0.4004 mL | 1.0009 mL | |
| 60 mM | 0.0334 mL | 0.1668 mL | 0.3336 mL | 0.8341 mL | |
| 80 mM | 0.0250 mL | 0.1251 mL | 0.2502 mL | 0.6256 mL | |
| 100 mM | 0.0200 mL | 0.1001 mL | 0.2002 mL | 0.5005 mL |