OATD-02 

OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC₅₀s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study^[1].

20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), 28 nM (rARG1)

OATD-02 inhibits mouse ARG in BMDM cells with IC₅₀ of 912.9 nM and human ARG2 in transfected CHO-K1 cells with IC₅₀ of 171.6 nM, and inhibits hARG1 in human primary hepatocytes at a much higher micromolar concentration (IC₅₀ = 13 mM) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

OATD-02 (10 mg/kg, oral gavage) generates a strong and a long pharmacodynamic effect in vivo, and has oral bioavailability of 13%, 30%, and 61% from mouse through rat to dog, respectively^[1].
OATD-02 (5 mg/kg, oral gavage) increases fourfold of the L-arginine concentration in plasma sustained even 1 week after end of a treatment^[1].
OATD-02 (twice per day at 50 mg/kg, oral gavage) inhibits the tumor growth in B16F10 orthotopic xenograft tumor model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

272.15

C₁₂H₂₅BN₂O₄

2146132-73-0

N[C@]1(C(O)=O)C[C@H](CCB(O)O)CC[C@H]1CN(C)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Borek B, et al. Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy. Mol Cancer Ther. 2023;22(7):807-817.  [Content Brief]