Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
説明 | 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]. |
In vitro | OATD-02 inhibits murine ARG in BMDM cells with an IC50 of 912.9 nM, human ARG2 in CHO-K1 cells with an IC50 of 171.6 nM, and hARG1 in primary human hepatocytes with an IC50 of 13 mM [1]. |
In vivo | OATD-02 (10 mg/kg, oral) exhibits strong, prolonged efficacy in vivo, with oral bioavailability observed at 13%, 30%, and 61% in mice, rats, and dogs, respectively [1]. When administered at 5 mg/kg orally, OATD-02 can maintain a fourfold increase in plasma L-arginine levels one week post-dosing [1]. Furthermore, bi-daily oral administration of OATD-02 at 50 mg/kg is capable of inhibiting the growth of B16F10 melanoma allografts in situ [1]. |
分子量 | 272.15 |
分子式 | C12H25BN2O4 |
CAS No. | 2146132-73-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
OATD-02 2146132-73-0 Immunology/Inflammation Arginase Inhibitor inhibitor inhibit