Catalog No.: PC-38628Not For Human Use, Lab Use Only.
OATD-01 (GLPG4716) is a highly potent, orally active chitotriosidase (CHIT1) inhibitor with IC50 of 26 (hCHIT1) and 29 nM (mCHIT1), inhibits hAMCase and mAMCase with IC50 of 9.0 and 7.8 nM, respectively.
OATD-01 (GLPG4716) is a highly potent, orally active chitotriosidase (CHIT1) inhibitor with IC50 of 26 (hCHIT1) and 29 nM (mCHIT1), inhibits hAMCase and mAMCase with IC50 of 9.0 and 7.8 nM, respectively.
OATD-01 poseeses binding affinity values for hCHIT1 (Ki=17.3 nM), mCHIT1 (Ki=26.05 nM), hAMCase (Ki= 4.8 nM), mAMCase (Ki=5.7 nM), and displays no inhibition against a panel of 98 targets in in vitro binding and enzymatic assays.
OATD-01 (30 and 100 mg/kg, p.o. q.d.) showed significant antifibrotic efficacy in an animal model of bleomycin-induced pulmonary fibrosis (IPF), decreased expression of profibrotic factors in lung tissues and reduced fibrosis and soluble collagen concentration.
