pf-9

PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM, and it inhibits IL-1β-induced PGE2 synthesis in vitro.

PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor with an IC50 of 420 nM and a Kd of 170 nM.

The dose-dependent effect of PF-915275 on the conversion of cortisone to cortisol in primary human and monkey hepatocytes (EC50: 20 and 100 nM, respectively). PF-915275 is an effective and selective human 11β-hydroxysteroid dehydrogenase type 1 inhibitor

PF-9601N showed high potency and selectivity as a MAO-BI (monoamine oxidase type B inhibitor) and also demonstrated remarkable neuroprotective properties in several in vivo and cellular models of PD.

PF-945863 is a macrolide antibiotic.

non-steroidal androgen receptor (AR) antagonist

PF-9404C is the S-S diesteroisomer of a beta adrenergic receptors blocker with vasodilatory properties. PF9404C increased the formation of cyclic GMP from 3 pmol mg−1 protein in basal conditions, to 53 pmol mg−1 protein in 10 μM in rat aorta smooth muscle

(Rac)-PF-998425 is a potent, selective, nonsteroidal androgen receptor (AR) antagonist with IC50 values of 26 nM in AR binding assays and 90 nM in cellular assays, respectively. This compound shows promise for investigating androgenetic alopecia.

PF-9363 (CTX-3648) is a potent and high selective KAT6A KAT6B inhibitor. PF-9363 can be used for the research of cancer.

ZY-19489 is an antimalarial compound that is a potential single-dose cure for Plasmodium falciparum and Plasmodium vivax malaria. It has received orphan drug designation from the FDA.

PF-00356231 hydrochloride is an inhibitor of matrix metalloproteinase MMP-12 with IC50 of 1.4 μM.

PF-06446846 hydrochloride, an orally active and highly selective inhibitor, targets Proprotein Convertase Subtilisin Kexin type 9 (PCSK9) translation by inducing ribosomal stalling at approximately codon 34, effectively suppressing PCSK9 expression.

Clesacostat (PF-05221304) is a potent and selective ACC inhibitor, with hACC1 IC50 of 13 nM and hACC2 IC50 of 9 nM. In animal models, PF-05221304 specifically inhibits hepatic DNL and demonstrates a significant safety margin for thrombocytopenia in non-human primate models.

GPR17 agonist

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neuronsin vivo.2It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose. 1.Claffey, M.M., Helal, C.J., Verhoest, P.R., et al.Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitorsJ. Med. Chem.55(21)9055-9068(2012) 2.Lai, B., Li, M., Hu, A., et al.The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learningDev. Neurobiol.78(9)859-872(2018)

PF-06815345 hydrochloride, an orally active potent inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9), has an IC50 value of 13.4 μM. It significantly decreases in vivo PCSK9 levels in mice.