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CAS No.: 344897-95-6

Leukadherin-1/白细胞粘附素-1 Catalog No. CSN19077

Synonyms: LA1

Leukadherin-1 is allosteric activator of CD11b/CD18 with EC50 value of 4 μM for increasing CD11b/CD18-dependent cell adhesion to fibrinogen.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

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.
动物研究
剂量
Mice: 0.4 mg/kg^[3] (i.p.), 2.5 mg/kg^[2] (i.p.); 1 mg/kg^[2] (i.v.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Mice: 0.4 mg/kg^[3] (i.p.), 2.5 mg/kg^[2] (i.p.); 1 mg/kg^[2] (i.v.)
给药途径	i.p., i.v.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3725 mL
- 11.8627 mL
- 23.7254 mL
- 5 mM
- 0.4745 mL
- 2.3725 mL
- 4.7451 mL
- 10 mM
- 0.2373 mL
- 1.1863 mL
- 2.3725 mL

技术信息

CAS号

344897-95-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H15NO4S2

运输

蓝冰

分子量

421.49

别名

LA1

溶解度

DMSO	15.0 mg/mL (35.6 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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Leukadherin-1/白细胞粘附素-1 Catalog No. CSN19077

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