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OATD-01

CAS No. : 2088453-21-6

MCE 站：OATD-01

产品活性：OATD-01 是一种高效、口服活性、 first-in-class、选择性几丁质酶 (chitinase) 抑制剂，对 CHIT1 具有低纳摩尔活性 (hCHIT1, IC₅₀=23 nM)。OATD-01 在多个物种中显示出良好的药代动力学特征。OATD-01 在体内具有显著的抗纤维化活性，用于肺纤维化 (IPF) 研究。

研究领域：Others

作用靶点：Others

In Vitro: OATD-01 exhibits high affinity toward h/mCHIT1 and h/mAMCase, and the inhibitory constants (K_i) for all four enzymes are 17.3 nM, 26.05 nM, 4.8 nM and 5.7 nM, respectively. These K_i values reveals good correlation with earlier established IC₅₀ data, the IC₅₀ values are 23 nM, 28 nM, 9 nM and 7.8 nM for hCHIT1,mCHIT1, hAMCase and mAMCase, respectively..
Off-target in vitro effects of compound OATD-01 have been evaluated at 10 μM in the Eurofins Panlabs panel of 98 in vitro binding and enzymatic assays, involving diverse molecular classes of proteins.

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-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 in this animal model.

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