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OATD-01

Chemical Structure : OATD-01

CAS No.: 2088453-21-6

OATD-01 (GLPG4716)

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.

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Biological Activity

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.

Physicochemical Properties

M.Wt 390.916
Formula C19H27ClN6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(4-((2S,5S)-5-(4-Chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-4H-1,2,4-triazol-3-amine

References

1. Koralewski R, et al. J Med Chem. 2020 Dec 24;63(24):15527-15540.

2. Sklepkiewicz P, et al. Eur J Pharmacol. 2022 Mar 15;919:174792.

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