GSK717

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Chemical Structure| 1595278-21-9 同义名 : -
CAS号 : 1595278-21-9
货号 : A1351257
分子式 : C28H28N4O2
纯度 : 99%
分子量 : 452.548
MDL号 : MFCD32671947
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(552.43 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：
生物活性
描述 As a NLR family member, NOD2 (nucleotide-binding oligomerization domain 2) is an intracellular pattern recognition receptor that assembles with receptor-interacting protein (RIP)-2 kinase in response to the presence of bacterial muramyl dipeptide (MDP) in the host cell cytoplasm, thereby inducing signals leading to the production of pro-inflammatory cytokines. GSK717 is a potent and selective NOD2 inhibitor. GSK717 (0.5-16 μM; 1 hour) blocked synergy between NOD2 and TLR2 (Toll-like receptor 2) in primary human monocytes. GSK717 does not affect NOD1, TNFR1 (tumour necrosis factor receptor-1) and TLR2-mediated responses. GSK717 (5 μM) inhibited the release of IL-8, IL-6, TNFα and IL-1β in primary human monocytes stimulated with MDP (muramyl dipeptide). GSK717 inhibited MDP-induced NOD2-mediated signaling with an IC50 of 400 nM for IL-8 secretion stimulated by MDP in HEK293/hNOD2 cells[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.05mL

2.21mL

1.10mL

22.10mL

4.42mL

2.21mL
参考文献

[1]Rickard DJ, et al. Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway. PLoS One. 2013;8(8):e69619. Published 2013 Aug 1.

[2]Rickard DJ, et al. Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway. PLoS One. 2013 Aug 1;8(8):e69619