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SR 1824 Sale

目录号 : GC14232

A non-agonist PPARγ ligand

SR 1824 Chemical Structure

Cas No.:1338259-06-5

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1mg
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Sample solution is provided at 25 µL, 10mM.

Description

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).

化学性质

Cas No. 1338259-06-5 SDF
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 SMILES BrC1=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°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.7197 mL 8.5985 mL 17.1969 mL
5 mM 0.3439 mL 1.7197 mL 3.4394 mL
10 mM 0.172 mL 0.8598 mL 1.7197 mL
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