Bioactivity | Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC50 of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling[1][2][3]. | ||||||||||||
Invitro | Leukadherin-1 is a specific agonist of the leukocyte surface integrin CD11b/CD18 (αMβ2; CR3; Mac-1). Leukadherin‐1 pretreatment reduces secretion of interferon (IFN)‐γ, tumour necrosis factor (TNF) and macrophage inflammatory protein (MIP)‐1β by monokine‐stimulated NK cells. Leukadherin‐1 pretreatment also reduces secretion of IL‐1β, IL‐6 and TNF by Toll‐like receptor (TLR)‐2 and TLR‐7/8‐stimulated monocytes[3]. | ||||||||||||
In Vivo | Leukadherin-1 (1 mg/kg; i.p.; twice daily for 14 days) is beneficial in preventing hyperoxia-induced neonatal lung injury, an experimental model of bronchopulmonary dysplasia (BPD)[1]. Animal Model: | ||||||||||||
Name | Leukadherin-1 | ||||||||||||
CAS | 344897-95-6 | ||||||||||||
Formula | C22H15NO4S2 | ||||||||||||
Molar Mass | 421.49 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
|
||||||||||||
Reference | [1]. Jagarapu J, et al. Efficacy of Leukadherin-1 in the Prevention of Hyperoxia-Induced Lung Injury in Neonatal Rats. Am J Respir Cell Mol Biol. 2015;53(6):793-801. [2]. Maiguel D, et al. Small molecule-mediated activation of the integrin CD11b/CD18 reduces inflammatory disease. Sci Signal. 2011;4(189):ra57. [3]. Roberts AL, et al. The complement receptor 3 (CD11b/CD18) agonist Leukadherin-1 suppresses human innate inflammatory signalling. Clin Exp Immunol. 2016;185(3):361-371. |