Lufotrelvir (PF-07304814)

Catalog No.S9858 Batch:S985801

Print

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
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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

Lufotrelvir (PF-07304814) is a phosphate prodrug of PF-00835231 that binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174 nM.
Targets
SARS-CoV-2 3CLpro
174 nM(Ki)
In vitro

As a phosphate prodrug of PF-00835231, Lufotrelvir (PF-07304814) shows strong antiviral activity by inhibiting coronavirus family 3CL protease activity, with no statistical difference in its antiviral potency in Vero cells expressing high levels of the efflux transporter P-glycoprotein.<sup><a class="sref" href="#s_ref">[1]</a></sup>
In Vivo

Lufotrelvir (PF-07304814) exhibits high conversion to PF-00835231, systemic clearance and short half-life across species in rats, dogs, and monkey, respectively. It also shows unbound CLint values of 51, 84, 168 and 428 µL/min/mg in rat, dog, monkey and human respectively.

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

    Using Lufotrelvir (PF-07304814), 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:

<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.

References

  • https://pubmed.ncbi.nlm.nih.gov/34663813/

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.