AUNP-12 acetate

AUNP-12 acetate rescued the proliferation in the mouse splenocyte assay system, with average EC50 values of 17 nM and 16.6 nM against rmPD-L1 and rmPD-L2 respectively. AUNP-12 (6 hours) showed a Plasma protein binding of 93.9% with plasma stability of more than 60%. AUNP-12 exhibited a half-life of 90 minutes in mouse liver microsomes. In male Balb/c mice, AUNP-12 subcutaneous injection or intravenous injection as a concentration of 3 mg/kg for its PK study. As a result, AUNP-12 shows a low volume of distribution, and the peak plasma levels reach at 0.2-0.4 hours. The absolute bioavailability of AUNP-12 is about 77% in mice. [1]

In vitro, AUNP-12 displayed equipotent antagonism toward PD-L1 and PD-L2 in the rescue of lymphocyte proliferation and effector functions. In human PBMC cells, AUNP-12 was also able to significantly rescue recombinant human PD-L1 and PD-L2 mediated inhibition in vitro, with average EC50 values of 63.3 nM and 44.1 nM against PD-L1 and PD-L2 respectively. [1]