|2-羟基-N,N,N-三甲基乙烷-1-氨基鎓(Z)-4-(5-((3-苄基-4-氧代-2-硫代噻唑烷-5-亚基)甲基)呋喃-2-基)苯甲酸盐|CsnPharm

CAS No.: 2055362-74-6

ADH-503 Catalog No. CSN24771

Synonyms: (Z)-Leukadherin-1 choline;Leukadherin-1 choline salt;LA1

ADH-503 is a potent agonist of the integrin CD11b to mitigate myeloid cell immunosuppression.

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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].
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.

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
- 1.9060 mL
- 9.5301 mL
- 19.0603 mL
- 5 mM
- 0.3812 mL
- 1.9060 mL
- 3.8121 mL
- 10 mM
- 0.1906 mL
- 0.9530 mL
- 1.9060 mL

技术信息

CAS号

2055362-74-6

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H28N2O5S2

运输

蓝冰

分子量

524.65

别名

(Z)-Leukadherin-1 choline;Leukadherin-1 choline salt;LA1

溶解度

DMSO	22.5 mg/mL (42.9 mM)
Water	2.1 mg/mL (4.0 mM)

动物实验配方

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