In vitro activity: HPGDS Inhibitor I (also known as H-PGDS inhibitor 1) is a novel, orally bioavailable, potent and selective inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS) with IC50 Value of 0.7 nM. The compound illustrated equal potency against purified HPGDS from human , rat, dog, and sheep with IC50 in the range of 0.5-2.3 nM. Hematopoietic prostaglandin D synthase (HPGDS) is primarly expressed in mast cells, antigen-presenting cells, and Th-2 cells. HPGDS converts PGH2 into PGD2, a mediator thought to play a pivotal role in airway allergy and inflammatory processes. HPGDS Inhibitor I reduces the antigen-induced response in allergic sheep.

Kinase Assay: HPGDS Inhibitor I (also known as H-PGDS inhibitor 1) is a novel, orally bioavailable, potent and selective inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS) with IC50 Value of 0.7 nM. The compound illustrated equal potency against purified HPGDS from human , rat, dog, and sheep with IC50 in the range of 0.5-2.3 nM.

Cell Assay: HPGDS inhibitor 1 was profiled in a panel of cellular assays to screen for activity against several relevant human enzyme targets. Those assay indicated that HPGDS inhibitor 1 does not inhibit human L- PGDS, m-PGDS, COX-1, COX-2 or 5 LOX (IC50 values> 10000 nM). HPGDS inhibitor 1 had a solubility of 1.5 ug/ml (3.9 uM) at pH 6.5.