| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
(Rac)-PF-998425 is a potent and selective antagonist of the Androgen Receptor (AR). As a nonsteroidal AR antagonist, it blocks the activation of AR signaling pathways, making it a valuable tool for investigating conditions driven by androgens, such as androgenetic alopecia.
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| ln Vitro |
(Rac)-PF-998425 demonstrates high potency in cell-free binding assays with an IC50 of 26 nM. It shows high selectivity for the AR and has minimal off-target activity at other steroid hormone receptors. This strong binding affinity forms the basis of its antagonistic activity in cellular systems.
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| ln Vivo |
In cellular assays, (Rac)-PF-998425 effectively antagonizes AR-mediated transcriptional activity with an IC50 of 90 nM. By blocking AR signaling in cells relevant to androgenetic alopecia, it inhibits the effects of dihydrotestosterone (DHT), the primary androgen involved in hair follicle miniaturization.
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| Enzyme Assay |
Cell-free AR binding assays are performed using a radioligand competition format. Purified human AR ligand-binding domain (LBD) is incubated with a high-affinity radiolabeled ligand (e.g., 3H-DHT) and varying concentrations of the test compound at 4degC for 12-16 hours. The bound and free fractions are separated by charcoal adsorption, and the half-maximal inhibitory concentration (IC50) is determined by scintillation counting.
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| Cell Assay |
Human dermal papilla cells (a key cell type involved in hair growth) are seeded in 96-well plates and cultured in growth medium. Cells are then treated with DHT (a potent androgen) and various concentrations of (Rac)-PF-998425 for 48-72 hours. The inhibition of androgen-induced growth suppression is assessed using a standard cell proliferation assay, such as CCK-8 or MTT, to measure antagonistic activity.
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| Animal Protocol |
Male C57BL/6 mice are a standard model for evaluating hair regrowth. After depilation to synchronize the hair cycle, animals are treated topically or systemically with (Rac)-PF-998425 while being challenged with DHT to induce hair loss. The effects on hair growth are evaluated by monitoring hair regrowth area, histological analysis of hair follicle density and morphology, and assessment of androgen-responsive gene expression in skin tissue.
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| ADME/Pharmacokinetics |
The pharmacokinetic (PK) profile of (Rac)-PF-998425 is being characterized to support its development as a topical or systemic agent. Studies are ongoing to evaluate its absorption through the skin, systemic exposure, and metabolism. Its favorable binding profile suggests it could be a promising candidate for formulation in dermatological research.
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| Toxicity/Toxicokinetics |
Toxicology studies are focused on local tolerance when applied to the skin. (Rac)-PF-998425 has shown a favorable safety profile in preliminary evaluations, with no significant systemic adverse effects. As a highly selective AR antagonist, it avoids the hormonal side effects often associated with less selective antiandrogens used in research.
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| References | |
| Additional Infomation |
Structure in the first source
(Rac)-PF-998425 is the racemic mixture of a research-use AR antagonist. Its high selectivity and potency make it a key tool for studying AR-driven pathways in both pre-clinical and cosmetic research settings. It is being investigated for applications beyond alopecia, including acne and other sebaceous gland disorders. It is for research use only and has not been approved for clinical use. |
| Molecular Formula |
C14H14F3NO
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|---|---|
| Molecular Weight |
269.2623
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| Exact Mass |
269.102
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| CAS # |
1076225-26-7
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| Related CAS # |
PF-998425;1076225-27-8
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| PubChem CID |
25093229
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| Appearance |
White to off-white solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
359
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1=C(C#N)C([H])=C([H])C(=C1[H])C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])O[H])(F)F
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| InChi Key |
MENRRRXHFQYXDW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H14F3NO/c15-14(16,17)12-7-9(5-6-10(12)8-18)11-3-1-2-4-13(11)19/h5-7,11,13,19H,1-4H2
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| Chemical Name |
4-(2-hydroxycyclohexyl)-2-(trifluoromethyl)benzonitrile
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (371.39 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7139 mL | 18.5694 mL | 37.1388 mL | |
| 5 mM | 0.7428 mL | 3.7139 mL | 7.4278 mL | |
| 10 mM | 0.3714 mL | 1.8569 mL | 3.7139 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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