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Chemical Structure| 1235403-62-9 Chemical Structure| 1235403-62-9

Structure of PF 05089771
CAS No.: 1235403-62-9

Chemical Structure| 1235403-62-9

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PF-05089771 is a Nav1.7 channel blocker with an IC50 of 8.6 nM.

4.5 *For Research Use Only !

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Product Details of PF 05089771

CAS No. :1235403-62-9
Formula : C18H12Cl2FN5O3S2
M.W : 500.35
SMILES Code : O=S(C1=CC(Cl)=C(OC2=CC=C(Cl)C=C2C3=CNN=C3N)C=C1F)(NC4=CSC=N4)=O
MDL No. :MFCD28900736
InChI Key :ZYSCOUXLBXGGIM-UHFFFAOYSA-N
Pubchem ID :46840946

Safety of PF 05089771

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Description
PF 05089771 is a potent, orally active, and selective arylsulfonamide Nav1.7 inhibitor, demonstrating IC50 values of 11 nM for hNav1.7, 12 nM for cynNav1.7, 13 nM for dogNav1.7, 171 nM for ratNav1.7, and 8 nM for musNav1.7. It is currently being investigated for potential applications in pain management and diabetic neuropathy[1][2].

In Vitro:

Cell Line
Concentration Treated Time Description References
Human embryonic kidney 293 cells 100-500 nM 10 minutes To study the inhibitory effect of PF-05089771 on Nav1.7 channels, results showed that 500 nM PF-05089771 produced steady-state inhibition of 95% ±2% in 10 minutes. Mol Pharmacol. 2020 Jun;97(6):377-383
Endometrial cancer cells 100 µM 48 hours PF-05089771 increased the number of early and late apoptotic cells and significantly attenuated the invasiveness of endometrial cancer cells. J Cancer. 2019 Aug 27;10(20):4954-4960

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice CFA-induced inflammation model Intraperitoneal injection 1 g/kg Single dose, behavioral testing performed 2 hours post-administration To evaluate the analgesic efficacy of PF-05089771 in an inflammation model. Results showed that PF-05089771 significantly reduced thermal and tactile sensitivity in CFA-inflamed mice but had no effect in control mice. Elife. 2024 Apr 30;12:RP90960
Mice Spinal cord injury model Intraperitoneal injection 2 mg/kg and 4 mg/kg From day 8 to day 11 after surgery PF-05089771 significantly alleviated mechanical pain in SCI mice at doses of both 2 mg/kg and 4 mg/kg, but 4 mg/kg did not increase the efficacy of pain relief. Front Mol Neurosci. 2023 Mar 3;16:1091096

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.00mL

0.40mL

0.20mL

9.99mL

2.00mL

1.00mL

19.99mL

4.00mL

2.00mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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