Identification | Back Directory | [Name]
OATD-01 | [CAS]
2088453-21-6 | [Synonyms]
OATD-01 inhibit,CHIT1,OATD-01,chitinase,antifibrotic,IPF,pulmonary fibrosis,OATD01,OATD 01,Inhibitor 1H-1,2,4-Triazol-3-amine, 5-[4-[(2S,5S)-5-[(4-chlorophenyl)methyl]-2-methyl-4-morpholinyl]-1-piperidinyl]- | [Molecular Formula]
C19H27ClN6O | [MDL Number]
MFCD33023453 | [MOL File]
2088453-21-6.mol | [Molecular Weight]
390.91 |
Chemical Properties | Back Directory | [Boiling point ]
586.4±60.0 °C(Predicted) | [density ]
1.297±0.06 g/cm3(Predicted) | [solubility ]
DMSO:100.0(Max Conc. mg/mL);255.81(Max Conc. mM) | [form ]
A solid | [pka]
12.86±0.40(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC50=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research[1]. | [in vivo]
OATD-01 (oral gavage; 30 mg/kg, 100 mg/kg; once daily; 21 days) shows significant antifibrotic efficacy in an animal model of Bleomycin (HY-108345)-induced pulmonary fibrosis. It reduces the degree of lung fibrosis in a dose-dependent manner, ultimately achieving comparable therapeutic efficacy to reference treatment with Nintedanib (HY-50904) in this animal model[1]. Animal Model: | Female BALB/c mice[1] | Dosage: | 30 mg/kg, 100 mg/kg | Administration: | Oral gavage; 30 mg/kg, 100 mg/kg; once daily; 21 days | Result: | Reduced the degree of lung fibrosis in vivo[1] |
| [References]
[1] Robert Koralewski, et al. Discovery of OATD-01, a First-in-Class Chitinase Inhibitor as Potential New Therapeutics for Idiopathic Pulmonary Fibrosis. J Med Chem. 2020 Dec 24;63(24):15527-15540. DOI:10.1021/acs.jmedchem.0c01179 |
|
Company Name: |
InvivoChem
|
Tel: |
13549236410 |
Website: |
https://www.invivochem.cn/ |
Company Name: |
|
Tel: |
4008-099-669 |
Website: |
http://m.is0513.com/ShowSupplierProductsList112975/0.htm |
|