HPGDS inhibitor 3_product_DataBase

Bioactivity	HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity[1].
Target	IC50: 9.4 nM (H-PGDS)EC50: 42 nM (H-PGDS)
In Vivo	HPGDS inhibitor 3 (compound 1y) (1-3 mg/kg; PO and IV; single) has a lower IV clearance, similar steady state volume of distribution, longer terminal half-life, and high oral bioavailability, as well as very low brain exposures in mouse, rat and dog[1].HPGDS inhibitor 3 (0.003-1 mg/kg; PO; single) attenuates PGD2 release to baseline levels in a dose-dependent manner; also inhibits LPS-induced PGD2 increase in plasma and skeletal muscle in a dose-dependent manner[1].HPGDS inhibitor 3 (0.003-1 mg/kg; PO; single) [1].HPGDS inhibitor 3 (1, 3, and 10 mg/kg; PO; q.d., for 16 days) significantly enhances functional recovery of injured limbs, and hastens the time to full functional recovery of injured limb muscles[1].HPGDS inhibitor 3 (10, 30 and 100 mg/kg; PO; once daily, for 7 days or 4 days) exhibits well tolerated at 30 mg/kg/day in rat but not tolerated at 100 mg/kg/day; shows well tolerated at 30 mg/kg/day in dogs but not tolerated at 75 mg/kg/day[1].Pharmacokinetic Parameters of HPGDS inhibitor 3 in mice, rats and dogs[1].
Name	HPGDS inhibitor 3
CAS	2255311-93-2
Formula	C21H27N3O2
Molar Mass	353.46
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Cadilla R, Deaton DN, Do Y, et al. The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure. Bioorg Med Chem. 2020;28(23):115791.

PeptideDB

HPGDS inhibitor 3

CAS: 2255311-93-2 F: C21H27N3O2 W: 353.46