Lufotrelvir (PF-07304814)

Catalog No.S9858 Batch:S985801

Technical Data

Formula	C₂₄H₃₃N₄O₉P
Molecular Weight	552.51	CAS No.	2468015-78-1
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (180.99 mM)
		Water	50 mg/mL (90.49 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

PF-07304814 is a phosphate prodrug of PF-00835231 that binds and inhibits SARS-CoV-2 3CL^pro activity with a Ki of 174 nM.

Targets

SARS-CoV-2 3CL^pro ^[1]

174 nM(Ki)

In vitro

Lufotrelvir (PF-07304814) is a phosphate prodrug of PF-00835231, and there is no statistical difference in antiviral potency of Lufotrelvir in vero cells expressing high levels of the efflux transporter P-glycoprotein, showing strong antiviral activity by inhibiting coronavirus family 3CL protease activity.<a class="sref" href="#s_ref">[1]</a>

In vivo

PF-07304814 exhibits high conversion to PF-00835231, systemic clearance and short half-life across species in rats, dogs, and monkey, respectively, also shows unbound CLint values of 51, 84, 168 and 428 µL/min/mg in rat, dog, monkey and human respectively. <a class="sref" href="#s_ref">[1]</a>

Protocol (from reference)

Cell Assay:^{<sup><a class="sref" href="#s_ref">[1]</a></sup>}	Cell lines VeroE6-ACE2 (Kideney), VeroE6-egfp (Kidney), A549-ACE2 (Lung) and MRC5 (Lung, h229E virus) Concentrations 0.01-1000 µM Incubation Time -- Method These cell lines were infected with the SARS-CoV-2 Washington strain 1 (WA1-EPI_ISL_404895) or the Belgium/GHB-03021/2020 strain (GHB-03021-EPI_ISL_407976), respectively, which have identical 3CL<sup>pro</sup> amino acid sequences and conducted with a cytopathic effect (CPE) assay.
Animal Study:^{<sup><a class="sref" href="#s_ref">[1]</a></sup>}	Animal Models Rat, dog, monkey and human Dosages 1.17 mg/kg for animals, 500 mg/day for human Administration i.v.

Cell Assay:^{<a class="sref" href="#s_ref">[1]</a>}

Cell lines
VeroE6-ACE2 (Kideney), VeroE6-egfp (Kidney), A549-ACE2 (Lung) and MRC5 (Lung, h229E virus)
Concentrations
0.01-1000 µM
Incubation Time
--
Method
These cell lines were infected with the SARS-CoV-2 Washington strain 1 (WA1-EPI_ISL_404895) or the Belgium/GHB-03021/2020 strain (GHB-03021-EPI_ISL_407976), respectively, which have identical 3CLpro amino acid sequences and conducted with a cytopathic effect (CPE) assay.

Animal Study:^{<a class="sref" href="#s_ref">[1]</a>}

Animal Models
Rat, dog, monkey and human
Dosages
1.17 mg/kg for animals, 500 mg/day for human
Administration
i.v.

References

[1] Britton Boras, et al. Nat Commun . 2021 Oct 18;12(1):6055.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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