Fluridil

Fluridil

FluridilDermatology
CAS: 260980-89-0
MF: C13H11F6N3O5
MW: 403.23
Indications
Alopecia Areata
Therapeutic Target
AR
Usage

A topical non-steroidal androgen receptor blocker with extremely low water solubility. Forms non-absorbable complexes on the skin surface, blocking androgen receptors with virtually no systemic absorption; classic safe topical anti-androgen used in hair tonics and scalp serums.

Specification
>99%
Product Description

Overview

Fluridil is a classic topical non-steroidal androgen receptor antagonist famous for its unique “becomes non-absorbable after application” design. Upon application, it rapidly forms stable, water-insoluble complexes on the scalp surface, effectively blocking androgen receptors while being almost 100% non-absorbed by the skin, resulting in near-zero systemic exposure and earning its reputation as the safest topical anti-androgen. Its core benefits include potent local anti-androgen action, no systemic side effects, excellent long-term safety, and significant slowing of androgenetic alopecia. Ideal for hair tonics, scalp serums, gels, and other topical anti-AGA products.

Synonyms: NP-619; Topilutamide; BP766; (2R)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]-3-[(2,2,2-trifluoroacetyl)amino]propanamide; PropanaMide,2-hydroxy-2-Methyl-N-[4-nitro-3-(trifluoroMethyl)phenyl]-3-[(2,2,2-trifluoroacetyl)aMino; 2-hydroxy-2-methyl-N-(4-nitro-3-(trifluoromethyl)phenyl)-3-(2,2,2-trifluoroacetamido)propanamide

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

Mol File: 260980-89-0.mol

Physicochemical Properties

Melting point: 144-145 °C

Boiling point: 284-289 °C

Density: 1.588±0.06 g/cm3(Predicted)

Storage temp.: Store at -20°C

Solubility: DMSO : 150 mg/mL (372.00 mM)

Form: Solid

Color: White to off-white

MSDS Information

Experimental Data

1.Cell Experiment

Solubility in DMSO: 100 mg/mL (248.00 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, 2 years; -20°C, 1 year. When stored at -80°C, use within 2 years; when stored at -20°C, use within 1 year.


2.Animal Experiment

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

For all of the following dissolution schemes, please first prepare a clear stock solution according to the In Vitro method, and then add solubilizing agents in sequence:


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

The percentages shown before the following solvents refer to the volume ratio of that solvent in the final solution you prepare. If precipitation or crystallization occurs during preparation, solubilization can be assisted by heating and/or sonication.


Protocol 1

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

Solubility: ≥ 2.5 mg/mL (6.20 mM); clear solution

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

For 1 mL of working solution as an example, take 100 μL of a 25.0 mg/mL clear DMSO stock solution and add it to 400 μL of PEG300, then mix well; next, add 50 μL of Tween-80 to the above mixture and mix thoroughly; then continue by adding 450 μL of saline and adjust the volume to 1 mL.

Preparation of saline: Dissolve 0.9 g of sodium chloride in ddH₂O and adjust the volume to 100 mL to obtain a clear, 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 (6.20 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 aqueous 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, transparent solution.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (6.20 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