OATD-01 是一种壳三糖苷酶及酸性哺乳动物几丁质酶的高活性抑制剂,对CHIT1具有低纳摩尔活性 (hCHIT1,IC50=23 nM)。它在多个物种中显示出良好的药代动力学特征,在体内具有显著的抗纤维化活性,可用于研究肺纤维化。
产品描述
OATD-01 is a highly active inhibitor of both Chitotriosidase (CHIT1) and acidic mammalian chitinase (AMCase).
体外活性
The Ki values for hCHIT1,mCHIT1, hAMCase and mAMCase are 17.3 nM, 26.05 nM, 4.8 nM and 5.7 nM, respectively[1]. These Ki values reveals good correlation with earlier established IC50 data, which are 23 nM, 28 nM, 9 nM and 7.8 nM, respectively[1]. OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets[1].
体内活性
OATD-01 given orally once daily in a range of doses between 30 and 100 mg/kg showed significant antifibrotic efficacy in an animal model of bleomycin-induced pulmonary fibrosis[1].
Cas No.
2088453-21-6
分子式
C19H27ClN6O
分子量
390.91
别名
OATD-01
储存和溶解度
DMSO:85 mg/ml (217.44 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years