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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产品名称 | Integrin ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tirofiban | ✔ | 99%+ | |||||||||||||||||
ATN-161 | ✔ | 98% | |||||||||||||||||
RGD | ✔ | 98% | |||||||||||||||||
A-205804 |
++
ICAM-1, IC50: 25 nM E-selectin, IC50: 20 nM |
98% | |||||||||||||||||
SB-273005 |
++++
αvβ5 receptor, IC50: 0.3 nM αvβ3 receptor, IC50: 1.2 nM |
98+% | |||||||||||||||||
Lifitegrast | ✔ | 97% | |||||||||||||||||
Cilengitide TFA |
+++
αvβ5 receptor, IC50: 79 nM αvβ3 receptor, IC50: 4.1 nM |
99%+ | |||||||||||||||||
Cyclo(-RGDfK) TFA | ✔ | 99%+ | |||||||||||||||||
Cyclo(RGDyK) trifluoroacetate |
++
αVβ3 integrin, IC50: 20 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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. |
Dose | Mice: 0.4 mg/kg[3] (i.p.), 2.5 mg/kg[2] (i.p.); 1 mg/kg[2] (i.v.) |
Administration | i.p., i.v. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 344897-95-6 |
分子式 | C22H15NO4S2 |
分子量 | 421.489 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
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 |