pf-9

GPR17 agonist

PF-9184 是一种有效且高度选择性的人微粒体前列腺素 E 合酶 1 (mPGES-1) 的抑制剂，IC50 值为 16.5 nM。PF-9184 体外抑制 IL-1β 诱导的 PGE2 合成。

PF9366 是甲硫氨酸腺苷转移酶 (Mat2A) 抑制剂，其 IC50=420 nM，Kd170 nM。

PF-915275 是口服有效的人 11β-羟基类固醇脱氢酶1型选择性抑制剂，Ki 为 2.3 nM，在 HEK293 细胞中的EC50为 15 nM 。它对人和猴原代肝细胞中可的松向皮质醇的转化具有剂量依赖性，EC50分别为 20 nM 和 100 nM。

PF-9601N 是一种单胺氧化酶 B (MAO-B) 抑制剂，在多种体内外模型中表现出抗帕金森病 (PD) 的神经保护作用。它可用于研究兴奋性毒性介导的神经退行性疾病。

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 antagonist of the androgen receptor (AR), with IC50 values of 26 nM and 90 nM in AR binding and cellular assays, respectively. This compound shows promise for investigating androgenetic alopecia.

PF-9363 (CTX-3648) 是一种有效且高选择性的 KAT6A KAT6B 抑制剂，可用于癌症研究。

PF-05180999 (PF-999) 是一种具有选择性和高效性的磷酸二酯酶 2A (PDE2A) 抑制剂，可在大鼠的情境恐惧条件反射模型中增强了长期记忆。

PF9238 is an inhibitor of beta-secretase I. PF9238 has a CatD potency of 12 uM in vivo.

F-95601 is a proton pump inhibitor.

ZY-19489是一种具有抗疟作用的化合物， 是一种潜在的单剂量根治性恶性疟原虫和间日疟原虫疟疾的药物，已获得美国 FDA 的孤儿药认定。

PF-00356231 hydrochloride 是基质金属蛋白酶 MMP-12 的抑制剂，IC50 为 1.4 μM。

PF-06446846 hydrochloride 是一种口服活性高、高选择性PCSK9(前蛋白转化酶枯草杆菌蛋白酶 kexin 9 型)翻译抑制剂。它通过在密码子34附近诱导核糖体暂停来抑制PCSK9。

Clesacostat（PF-05221304），是一种高效且选择性的ACC抑制剂（hACC1 IC50 = 13nM；hACC2 IC50 = 9nM）。在动物模型中，PF-05221304特异性抑制肝脏的DNL，同时在非人类灵长类动物模型中展示出对血小板减少具有显著的安全裕度。

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 是一款口服有效的PCSK9抑制剂，其IC50值为13.4 μM。在小鼠体内，能显著降低PCSK9水平。