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OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase 1 and Arginase 2 that exhibits slow dissociation kinetics and nanomolar potency across human and murine arginases, effectively reversing arginase-mediated tumor immunosuppression and enabling mechanistic studies in melanoma immunotherapy research.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | Inquiry | 8-10 weeks | 8-10 weeks | |
| 50 mg | Inquiry | 8-10 weeks | 8-10 weeks |
| Description | OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase 1 and Arginase 2 that exhibits slow dissociation kinetics and nanomolar potency across human and murine arginases, effectively reversing arginase-mediated tumor immunosuppression and enabling mechanistic studies in melanoma immunotherapy research. |
| Targets&IC50 | Arginase (mouse):912.9 nM, Arginase II (human):171.6 nM |
| In vitro | In enzymatic assays, OATD-02 inhibited recombinant human ARG1/ARG2 (IC50 20/39 nM) and rodent ARG1 variants. In cellular models, it inhibited human ARG2 in CHO-K1 cells (IC50 171.6 nM) and mouse ARG in bone marrow macrophages (IC50 912.9 nM), while showing a significantly higher IC50 (13 mM) for ARG1 in human primary hepatocytes [1]. |
| In vivo | Oral administration of OATD-02 (10 mg/kg) demonstrates bioavailability of 13% in mice, 30% in rats, and 61% in dogs. A dosage of 5 mg/kg maintained a 4-fold increase in plasma L-arginine levels one week after treatment cessation. In a B16F10 orthotopic melanoma model, treatment with OATD-02 (50 mg/kg, twice daily, p.o.) for 15 days resulted in a Tumor Growth Inhibition (TGI) of 46% [1]. |
| Synonyms | OATD02, OATD 02 |
| Molecular Weight | 272.15 |
| Formula | C12H25BN2O4 |
| Cas No. | 2146132-73-0 |
| Smiles | C(O)(=O)[C@]1(N)[C@H](CN(C)C)CC[C@@H](CCB(O)O)C1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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