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Leukadherin-1

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Chemical Structure| 344897-95-6 同义名 : -
CAS号 : 344897-95-6
货号 : A292458
分子式 : C22H15NO4S2
纯度 : 98%
分子量 : 421.489
MDL号 : MFCD01151276
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 4 mg/mL(9.49 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 The β2 integrin CD11b/CD18 (also known as Mac-1, aMb2, and CR3),expressed primarily in the cells of the innate immune system,is a key adhesion receptor that mediates leukocyte migration and immune functions. ICAM-1 (CD54),a member of the immunoglobulin family,is expressed on the surface of vascular endothelial cells and mediates migration and tissue recruitment of leukocytes from circulation. Leukadherin-1 (LA1) is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1. Daily LA1 intraperitoneal treatment at 2.5 mg/kg reduced interstitial leukocyte infiltration in the kidney allograft, reduced neointimal hyperplasia and glomerular damage, and prolonged graft survival from 48.5% (CsA only) to 100% (CsA and LA1) on day 60[3]. LA1 pre-treatment at 7.5 mM reduced secretion of IFN–γ, TNF and MIP-1β by monokine-stimulated Natural Killer (NK) cells which was associated with a decrease in pSTAT5 following IL-12+IL-15 stimulation (P<0.02) and increased IL-10 secretion following IL-12+IL-18 stimulation (P<0.001). Also, LA1 pre-treatment reduced secretion of IL-1β, IL-6 and TNF by Toll-like receptor (TLR) 2 and TLR7/8–stimulated monocytes[4].
作用机制 Leukadherin-1 enhances binding of CD11b/CD18 to ICAM-1 via the formation of long membrane tethers.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.86mL

2.37mL

1.19mL

23.73mL

4.75mL

2.37mL

参考文献

[1]Roberts AL, Furnrohr BG, et al. The complement receptor 3(CD11b/CD18) agonist Leukadherin-1 suppresses human innate inflammatory signalling. Clin Exp Immunol. 2016 Sep;185(3):361-71.

[2]Khan SQ, Guo L,et al. A Small Molecule β2 Integrin Agonist Improves Chronic Kidney Allograft Survival by Reducing Leukocyte Recruitment and Accompanying Vasculopathy. Front Med (Lausanne). 2014 Nov 12;1:45.

[3]Khan SQ, Guo L, Cimbaluk DJ, Elshabrawy H, Faridi MH, Jolly M, George JF, Agarwal A, Gupta V. A Small Molecule β2 Integrin Agonist Improves Chronic Kidney Allograft Survival by Reducing Leukocyte Recruitment and Accompanying Vasculopathy. Front Med (Lausanne). 2014 Nov 12;1:45. doi: 10.3389/fmed.2014.00045. PMID: 25593918; PMCID: PMC4291902.

[4]Roberts AL, Fürnrohr BG, Vyse TJ, Rhodes B. The complement receptor 3 (CD11b/CD18) agonist Leukadherin-1 suppresses human innate inflammatory signalling. Clin Exp Immunol. 2016 Sep;185(3):361-71. doi: 10.1111/cei.12803. Epub 2016 Jul 26. PMID: 27118513; PMCID: PMC4991522.