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OATD-02

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Catalog No. T79319Cas No. 2146132-73-0

OATD-02 is an orally active, competitive, reversible, noncovalent inhibitor with slow offset kinetics that targets both Arginase1 and Arginase2, 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].

OATD-02

OATD-02

😃Good
Catalog No. T79319Cas No. 2146132-73-0
OATD-02 is an orally active, competitive, reversible, noncovalent inhibitor with slow offset kinetics that targets both Arginase1 and Arginase2, 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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5 mgInquiry8-10 weeks
50 mgInquiry8-10 weeks
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Product Introduction

Bioactivity
Description
OATD-02 is an orally active, competitive, reversible, noncovalent inhibitor with slow offset kinetics that targets both Arginase1 and Arginase2, 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) demonstrates strong, prolonged in vivo efficacy, with oral bioavailability at 13%, 30%, and 61% in mice, rats, and dogs, respectively [1]. At 5 mg/kg orally, it maintains a fourfold increase in plasma L-arginine levels one week post-dosing [1]. Bi-daily oral administration at 50 mg/kg inhibits B16F10 melanoma allograft growth [1].
Chemical Properties
Molecular Weight272.15
FormulaC12H25BN2O4
Cas No.2146132-73-0
Storage & Solubility Information
StorageShipping with blue ice.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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