产品说明书

ADH-503

Print
Chemical Structure| 2055362-74-6 同义名 : (Z)-Leukadherin-1 choline;GB1275
CAS号 : 2055362-74-6
货号 : A1193403
分子式 : C27H28N2O5S2
纯度 : 98%
分子量 : 524.652
MDL号 : N/A
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 20 mg/mL(38.12 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

无水乙醇: 3 mg/mL(5.72 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
描述 CD11b/CD18 is a dimeric integrin highly expressed on the surface of myeloid cells and plays an important role in transendothelial migration and tissue recruitment during inflammatory immune responses. ADH-503 is a small-molecule allosteric agonist of CD11b/CD18 that partially actives CD11b conformation through binding. It increased CD11b/CD18-dependent cell adhesion to fibrinogen with an EC50 value of 4 mM. Treatment of leukocytes with 15 μM ADH-503 led to a significant decrease in lateral migration and migration velocity compared to DMSO-treated controls. The intravital microscopic analysis of mouse cremaster muscle showed that ADH-503 at 100 μM decreased the rolling velocity of leukocytes in TNF-α-treated venules. In a mouse model of acute, thioglycolate-induced peritonitis, administration of ADH-503 (200 μL of a 50 μM solution in saline) 30 min before thioglycolate injection reduced the amount of neutrophil accumulation by 40% compared to vehicle-pretreated mice. Also, neutrophil accumulation in ADH-503-treated mice was reduced at 4 h after thioglycolate injection and stayed reduced at 12 h[1].
作用机制 ADH-503 is a small-molecule agonist of CD11b/CD18 that preferentially binds to the open conformation of the αA domain in CD11b/CD18, thereby allosterically stabilizing the αA domain in its high-affinity conformation and activating CD11b/CD18[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.53mL

1.91mL

0.95mL

19.06mL

3.81mL

1.91mL
参考文献

[1]Maiguel D, Faridi MH, Wei C, et al. Small molecule-mediated activation of the integrin CD11b/CD18 reduces inflammatory disease. Sci Signal. 2011;4(189):ra57.