ADH-503;ADH503;ADH 503

生物活性靶点体外研究体内研究 ADH-503;ADH503;ADH 503 试剂级价格

CAS号:2055362-74-6
英文名:ADH-503
中文名:ADH-503;ADH503;ADH 503
CBNumber:CB35582357
分子式:C27H29N2O5S2+
分子量:525.66
MOL File:2055362-74-6.mol

ADH-503;ADH503;ADH 503化学性质

储存条件 :Store at -20°C
溶解度 :DMSO: 21.43 mg/mL (40.85 mM)
形态 :Solid
颜色 :Brown to reddish brown

ADH-503;ADH503;ADH 503性质、用途与生产工艺

生物活性 ADH-503 ((Z)-Leukadherin-1 choline) 是一种具有口服活性的，变构的 CD11b 激动剂。ADH-503 可以导致与肿瘤相关的巨噬细胞重新极化，减少肿瘤浸润性免疫抑制骨髓细胞的数量，并增强树突状细胞的反应。
靶点

CD11b
体外研究

ADH-503 ((Z)-Leukadherin-1 choline; 4 μM; 8 days) reduces the numbers of total tumor-infiltrating CD11b ⁺ cells and subsets of CD11b ⁺ monocytes, granulocytes, eosinophils, and macrophages.

体内研究

ADH-503 ((Z)-Leukadherin-1 choline; 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.
ADH-503 (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 AUC _0-t in the plasma of 6950 and 13962 ng.h/mL at 30 and 100 mg/kg dosing, respectively.

Animal Model:	KPC mice [p48-CRE/Lox-stop-Lox(LSL)-Kras ^G12D /p53 ^flox/flox ]
Dosage:	30, 60, or 120 mg/kg
Administration:	Oral gavage; 60 days
Result:	Delayed tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival.

Animal Model:	Male rats
Dosage:	30, 100 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral gavage twice a day; on days 1 and 5
Result:	Had the mean half-life of 4.68 and 3.95 hours, 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.