OATD-02 is an orally active, competitive, reversible, noncovalent inhibitor with slow offset kinetics that targets both Arginase1 and 2, exhibiting inhibitory concentrations (IC50) of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1). Notably, OATD-02 mitigates tumor immunosuppression provoked by these arginases and has potential application in melanoma research [1].

OATD-02在BMDM细胞中抑制小鼠ARG的IC50值为912.9 nM，在CHO-K1细胞中对人ARG2展示的IC50为171.6 nM，且在人原代肝细胞中对hARG1的IC50达13 mM。[1]

OATD-02 (10 mg/kg, 口服) 在动物模型中显示出长期的药效，其口服生物利用度在小鼠、大鼠及犬体内分别达到 13%、30% 与 61% [1]。此外，OATD-02 (5 mg/kg, 口服) 能够在给药一周后使血浆中的L-精氨酸浓度提高至四倍 [1]。在每日两次给予OATD-02 (50 mg/kg, 口服) 的情况下，能有效抑制B16F10原位移植肿瘤的生长 [1]。