OATD-01 (GLPG4716)

Chemical Structure : OATD-01

CAS No.: 2088453-21-6

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货号: 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.

规格	价格	库存
5 mg	￥1280	In stock
10 mg	￥1980	In stock
25 mg	￥3480	In stock
50 mg	￥5580	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	390.916
分子式	C19H27ClN6O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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.

OATD-01 (GLPG4716)

生物&药学活性

物理化学性质&存储条件

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OATD-01 (GLPG4716)

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