| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C12H25BN2O4 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase 1 and 2. As a slow-offset inhibitor, it blocks intracellular arginases with IC50 values of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1) and 28 nM (rARG1). It reverses tumor immunosuppression driven by both arginases and can be used for melanoma studies[1]. It has a molecular formula of C12H25BN2O4 and a molecular weight of 272.15 g/mol.
Physical & Chemical Properties
| CAS Number | 2146132-73-0 |
|---|---|
| Molecular Formula | C12H25BN2O4 |
| Molecular Weight | 272.15 g/mol |
| SMILES | N[C@]1(C(O)=O)C[C@H](CCB(O)O)CC[C@H]1CN(C)C |
| Signaling Pathway | Immunology/Inflammation; Metabolic Enzyme/Protease |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), 28 nM (rARG1)
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
OATD-02 inhibits mouse ARG in BMDM cells (IC50 = 912.9 nM) and human ARG2 in transfected CHO-K1 cells (IC50 = 171.6 nM); in human primary hepatocytes, hARG1 is inhibited at a much higher micromolar concentration (IC50 = 13 μM)[1].
In Vivo
OATD-02 (10 mg/kg, oral gavage) produces a strong and long pharmacodynamic effect in vivo, and its oral bioavailability is 13% in mouse, 30% in rat, and 61% in dog[1]. OATD-02 (5 mg/kg, oral gavage) raises the plasma L-arginine concentration fourfold, and this is sustained even 1 week after the end of treatment[1]. OATD-02 (twice per day at 50 mg/kg, oral gavage) inhibits tumor growth in the B16F10 orthotopic xenograft tumor model[1].
| Animal Model | B16F10 orthotopic xenograft tumor model[1] |
|---|---|
| Dosage | Twice per day at 50 mg/kg for 15days |
| Administration | Oral gavage |
| Result | Inhibited tumor growth (TGI 46%). |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Blockade of CCR5+ T Cell Accumulation in the Tumor Microenvironment Optimizes Anti-TGF-β/PD-L1 Bispecific Antibody. Adv Sci (Weinh) 2024 Nov;11(43):e2408598. PMID: 39303165
