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SR 1824
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SR 1824图片
CAS NO:1338259-06-5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Cas No.1338259-06-5
化学名(S)-4'-((5-((1-(4-bromophenyl)ethyl)carbamoyl)-2,3-dimethyl-1H-indol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid
Canonical SMILESBrC1=CC=C([C@H](C)NC(C2=CC=C(N(CC3=CC=C(C4=CC=CC=C4C(O)=O)C=C3)C(C)=C5C)C5=C2)=O)C=C1
分子式C33H29BrN2O3
分子量581.5
溶解度≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ki = 10 nM

SR 1824 is a non-agonist PPARγ ligand.

Peroxisome proliferator-activated receptor γ (PPARγ) can be activated by the anti-diabetes drugs known as thiazolidinediones, including rosiglitazone and pioglitazone. Phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) leads to dysregulation of genes whose expression is altered in obesity, such as adiponectin.

In vitro: In a previous study, SR1824 was characterized for its ability to block Cdk5-dependent phosphorylation of PPARγ. The results demonstrated that SR1824 could potently block Cdk5-dependent phosphorylation of PPARc in cells while displaying little to no classical agonism. In the docking study, the HDX analyses showed that SR1824 and its analog of SR1664 werer able to increase the conformational mobility of the C-terminal end of H11, a helix that abuts H12; in contrast, the full and partial agonists could stabilize the same region of H11. Morover, as expected SR1664 and SR1824 did not interact with H12 in any detectable way, but unexpectedly both ligands cause an increase in the conformational mobility of H11, which was part of the AF2 surface and directly abuts H12 [1].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Choi, J. H.,Banks, A.S.,Kamenecka, T.M., et al. Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation. Nature 477(7365), 477-481 (2011).