PF-998425

• CAT Number: R055642
• CAS Number: 1076225-27-8
• Molecular Formula: C14H14F3NO
• Molecular Weight: 269.26
• Purity: ≥95%
• Synonyms: 4-[(1R,2R)-2-hydroxycyclohexyl]-2-(trifluoromethyl)benzonitrile
• InChI: 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/t11-,13-/m1/s1
• InChIKey: MENRRRXHFQYXDW-DGCLKSJQSA-N
• SMILES: C1CCC(C(C1)C2=CC(=C(C=C2)C#N)C(F)(F)F)O

PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC50 of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research[1].
PF-998425 (Compound (-)-6a) is rapidly metabolized in rat liver microsomes (t1/2=4 min, CLint=350 (µL/min)/mg protein). In vivo clearance data in dogs are consistent with the high clearance predicted in vitro in rat. Following intravenous administration of PF-998425, mean systemic plasma clearance is 40 (mL/min)/kg. The mean apparent of volume of distribution at steady state is 6.5 L/kg, and the mean terminal phase half-life is 2.6 h[1].

Reference

[1]. Jie Jack Li, et al. Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications. J Med Chem. 2008 Nov 13;51(21):7010-4.
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