(Z)-Leukadherin-1

2055362-72-4

421.49

10 mM in DMSO

Immunology/Inflammation

(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (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]. IC50 & Target: CD11b^[1] In Vitro: (Z)-Leukadherin-1 (ADH-503 free base; 4 uM; 8 days) reduces the numbers of total tumor-infiltrating CD11b⁺ cells and subsets of CD11b⁺ monocytes, granulocytes, eosinophils, and macrophages^[1]. In Vivo: (Z)-Leukadherin-1 (ADH-503 free base; oral gavage; 30, 60, or 120 mg/kg; twice a day for 60 days) delayes tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival^[1].
(Z)-Leukadherin-1 (oral gavage; 30, 100 mg/kg; twice a day; on days 1 and 5) has the mean half-life of 4.68 and 3.95 hours, a maximum concentration of 1716 and 2594 ng/ml and AUC0-t in the plasma of 6950 and 13962 ng.h/ml at 30 and 100 mg/kg dosing, respectively^[1].