Pemetrexed disodium(培美曲塞二钠) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively.
MK-8245 is an liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.
Leflunomide(来氟洛米) is a pyrimidine synthesis inhibitor belonging to the DMARD, used as an immunosuppressant agent.
Dorzolamide HCl(盐酸多佐胺) is a water-soluble, potent inhibitor of human carbonic anhydrase II and IV with Ki of 1.9 nM and 31 nM, respectively, used as anti-glaucoma agent.
It was developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more.
The PDE4 selective inhibitor, rolipram(咯利普兰), inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively an anti-inflammatory agent.
Zileuton(齐留通) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma.
Cilomilast(西洛司特) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity.