HPGDS-inhibitor-1

Cas No.:	1033836-12-2
Chemical Name:	4-Amino-7-chloroquinazoline
Synonyms:	4-Amino-7-chloroquinazoline;6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)-4-piperidinyl]-3-Pyridinecarboxamide;6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide;HPGDS inhibitor 1;HPGDS Inhibitor I;HPGDS-inhibitor-1;Prostaglandin D Synthase (hematopoietic-type) Inhibitor I;6-(3-fluorophenyl)-N-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)nicotinaMide;3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]-
SMILES:	O=C(NC1CCN(CC(F)(F)F)CC1)C2=CC=C(C3=CC=CC(F)=C3)N=C2
Formula:	C19H19N3OF4
M.Wt:	381.36726
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.IC50 Value: 0.7 nM [1]Target: HPGDSHPGDS inhibitor 1 was elected for further profiling based on its enzyme and cell potency. The compound illustrated equal potency against purified HPGDS from human , rat, dog, and sheep (IC50, 0.5-2.3 nM). 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. The compound had excellent PK characteristics when dosed in rats at 1 mpk with 76% bioavailavility. Rats dosed orally with 1 and 10 mpk HPGDS inhibitor 1 were sacrificed at various times, and plasma concentrations of HPGDS inhibitor 1 and spleen PGD2 concentrations were measured. Oral administration of HPGDS inhibitor 1 blocked PGD2 production in the rat spleen; inhibition of PGD2 was inversely correlated with the plasma concentration of HPGDS inhibitor 1 in a time and dose-dependent manner. Spleen PGD2 levels fall as HPGDS inhibitor 1 plasma levels increase over time; PGD2 levels return to baseline levels as HPGDS inhibitor 1 plasma levels decline.