PF-998425

PF-998425

PF-998425Dermatology
CAS: 1076225-27-8
MF: C14H14F3NO
MW: 269.26
Indications
Alopecia
Therapeutic Target
AR
Usage

A potent non-steroidal androgen receptor antagonist that blocks DHT binding at the follicle level without entering the bloodstream or affecting systemic hormones; new-generation core ingredient for androgenetic alopecia, used in premium hair growth serums and ampoules.

Specification
>99%
Product Description

Overview

PF-998425 is a next-generation potent non-steroidal androgen receptor antagonist distinguished by its “purely local action, zero systemic absorption” profile, making it the most ideal core anti-AGA ingredient available today. It completely blocks DHT–androgen receptor binding directly at the follicle level with virtually no bloodstream entry or disruption of systemic hormones, offering exceptional safety. Its key benefits include anti-androgen efficacy comparable to finasteride, zero hormonal side effects, rapid blockade of androgen signaling, and significant slowing of AGA progression. Perfect for premium anti-androgen hair growth serums, ampoules, and professional scalp treatments.

Synonyms: PF998425; 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile; rel-(-)-4-[(1R,2R)-2-Hydroxycyclohexyl]-2-(trifluoroMethyl)benzonitrile; Benzonitrile,4-[(1R,2R)-2-hydroxycyclohexyl]-2-(trifluoromethyl)-

Product Categories: Non-Steroidal Androgen Receptor Antagonists; Androgen Receptor Antagonists; Topical Antiandrogens

Mol File: 1076225-27-8.mol

Physicochemical Properties

Boiling point: 365.2±42.0 °C(Predicted)

Density: 1.28±0.1 g/cm3(Predicted)

Storage temp.: Store at +4°C

Solubility: DMSO: ≥10mg/mL

Form: Powder

Color: White to off-white

MSDS Information

Experimental Data

1.Cell Experiment

Solubility in DMSO: 50 mg/mL (185.69 mM; assisted by sonication; hygroscopic DMSO significantly affects the solubility of the product, please use freshly opened DMSO)

Preparing Stock Solutions:

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Please choose a suitable solvent to prepare the stock solution based on the product's solubility in different solvents. Once the solution is prepared, aliquot and store it to avoid product degradation caused by repeated freeze-thaw cycles.

Storage conditions and shelf life of the stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, use within 6 months; when stored at -20°C, use within 1 month.


2.Animal Experiment

Please choose the appropriate dissolution method based on your experimental animals and administration route.

For the following dissolution solutions, please first prepare a clear stock solution according to the In Vitro method, then add solubilizers in sequence:

—— To ensure the reliability of the experimental results, the clear stock solution can be appropriately stored based on storage conditions; for in vivo experimental working solutions, it is recommended to prepare them fresh and use them on the same day;  

The percentages shown before each solvent below refer to the volume proportion of that solvent in the final solution you are preparing; if precipitation or crystallization occurs during preparation, solubilization can be assisted by heating and/or ultrasonic treatment.


Protocol 1

Please add each solvent in sequence: 10% DMSO, 40% PEG300, 5% Tween-80, 45% Saline.

Solubility: 2.5 mg/mL (9.28 mM); suspension; ultrasound-assisted solubilization.

This method can produce a uniform suspension at 2.5 mg/mL, which can be used for oral administration and intraperitoneal injection.

Taking 1 mL of working solution as an example, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 to the above mixture and mix thoroughly; finally, add 450 μL of saline to bring the volume to 1 mL.

Preparation of saline: Dissolve 0.9 g of sodium chloride in ddH₂O and make up to 100 mL to obtain a clear and transparent saline solution.

Protocol 2

Please add each solvent in order: 10% DMSO, 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (9.28 mM); clear solution

This protocol can yield a clear solution with ≥ 2.5 mg/mL (saturation unknown).

For 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD saline solution and mix well.

Dissolve 2 g of SBE-β-CD (sulfobutyl ether β-cyclodextrin) powder in 10 mL of saline, fully dissolving to a clear and transparent solution.

Protocol 3

Please add each solvent in order: 10% DMSO, 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (9.28 mM); clear solution

This method can produce a clear solution with ≥ 2.5 mg/mL (saturation unknown). For animal experiments lasting more than half a month, use this method as appropriate.

For 1 mL of working solution, take 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of corn oil, then mix thoroughly.

Pharmacodynamics

Mechanism Of Action