BML-111, a lipoxin A4 analog, is a lipoxin A4 receptor agonist. BML-111 represses the activity of angiotensin converting enzyme (ACE) and increases the activity of angiotensinconverting enzyme 2 (ACE2). BML-111 has antiangiogenic, antitumor and anti-inflammatory properties.
体外研究
In H22 cells, BML-111 inhibits the production of vascular endothelial growth factor and reduces hypoxia-inducible factor-1α level.
BML-111 inhibits leukotriene B4-induced cellular migration with an IC50 of 5 nM.
体内研究
BML-111 (1 mg/kg; intraperitoneal injection; for 15 days; male Imprinting Control Region mice) treatment suppresses tumor-related angiogenesis and tumor growth in vivo. BML-111 also enhances the in situ apoptosis while inhibiting macrophage infiltration in tumor tissue.
BML-111 protects LPS-induced acute lung injury and LPS/D-GalN-induced acute liver injury. BML-111 represses the activity of ACE, but increases the activity of ACE2. BML-111 decreases the expression levels of ACE, AngII, and AngII type 1 receptor (AT1R), meanwhile increases the levels of ACE2, angiotensin-(1-7) (Ang-1-7), and Mas.
Animal Model:
Male Imprinting Control Region mice (5-6-week-old,18-22 g) injected with H22 cells
Dosage:
1 mg/kg
Administration:
Intraperitoneal injection; injected 5 minutes before and 4 hours after H22 cell inoculation, then every 12 hours for 2 consecutive days, then daily in an additional 3 days and every other day for the last 10 days
Result:
Suppressed tumor-related angiogenesis and tumor growth in vivo.
分子式
C8H16O5
分子量
192.21
CAS号
78606-80-1
运输条件
Room temperature in continental US; may vary elsewhere.