(Z)-LeukadHERin-1 是 CD11b 的变构激动剂。

(Z)-Leukadherin-1 is an allosteric agonist of CD11b.

(Z)-Leukadherin-1 (4 μM) treatment reduces the numbers of total tumor-infiltrating CD11b+ cells and subsets of CD11b+ monocytes, eosinophils, granulocytes, and macrophages. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses[1].

(Z)-Leukadherin-1 shows a mean half-life of 4.68 and 3.95 h, a maximum concentration of 1716 and 2594 ng/ml and AUC(0-t) in the plasma of 6950 and 13962 ng·h/ml at 30 and 100 mg/kg dosing, respectively. In KPC mice, (Z)-Leukadherin-1 (30, 60, or 120 mg/kg; gavage) delayes tumor progression and leads to a significantly decreased tumor burden in time-point analysis and improved overall survival[1].

2055362-72-4

C22H15NO4S2

421.49

ADH-503 free base

DMSO:4 mg/mL (9.49 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years