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首页-小分子抑制剂&激动剂-Cytoskeleton/Cell Adhesion Molecules-Integrin-GW559090
GW559090

Chemical Structure : GW559090

CAS No.: 278598-52-0

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GW559090 (GW 559090)

货号: PC-49182Not For Human Use, Lab Use Only.

GW559090 is a potent, selective, competitive and high-affinity α4β1 integrin (VLA-4) antagonist with Kd of 0.19/1.04 nM for huamn/rat α4β1, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GW559090 is a potent, selective, competitive and high-affinity α4β1 integrin (VLA-4) antagonist with Kd of 0.19/1.04 nM for huamn/rat α4β1, respectively.
GW559090 inhibits J6 cell adhesion to VCAM-1 in a monophasic fashion with a mean IC50 of 7.72 nM (2.39-24.9 nM), inhibits RPMI 8866 cell adhesion to MAdCAM with an IC50 of 23.0 nM, inhibits RPMI 8866 binding to VCAM-1, and CS-1 in a simple monophasic manner with respective IC50s of 4.81 nM and 24.5 nM.
GW559090 displays no significant inhibition on 53 receptors and 4 transporters in an MDS Pharma screen, including LFA-1.
GW559090 (topical treatment, 30 mg/mL) dose-dependently prevents desiccation-induced corneal barrier disruption, decreases dendritic cell activation in lymph nodes. reduces corneal expression of IL-1α, matrix metalloproteinase (MMP)-9, chemokine ligand 9 (CXCL9), and TGF-β1.
GW559090 acts primarily locally, not systemically, to improve DS-induced corneal barrier disruption.

物理化学性质&存储条件

分子量 596.681
分子式 C31H40N4O8
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-3-(4-((4-carbamoylpiperidine-1-carbonyl)oxy)phenyl)-2-((S)-4-methyl-2-(2-(o-tolyloxy)acetamido)pentanamido)propanoic acid

参考文献

1. Achim H Krauss, et al. Invest Ophthalmol Vis Sci. 2015 Sep;56(10):5888-95.

2. Chen YH, et al. J Neuroinflammation. 2021 Feb 18;18(1):49.

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