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OATD-02

Catalog No. T79319   CAS 2146132-73-0

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].

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OATD-02 Chemical Structure
OATD-02, CAS 2146132-73-0
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Biological Description
Chemical Properties
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Description 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].
Molecular Weight 272.15
Formula C12H25BN2O4
CAS No. 2146132-73-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

OATD-02 2146132-73-0 Immunology/Inflammation Arginase inhibitor inhibit

 

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