4′-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]- [1,1′-Biphenyl]-2-carboxylic acid
- Product Name
- 4′-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]- [1,1′-Biphenyl]-2-carboxylic acid
- CAS No.
- 1338259-05-4
- Chemical Name
- 4′-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]- [1,1′-Biphenyl]-2-carboxylic acid
- Synonyms
- SR1664;SR1664 >=98% (HPLC);SR1664, 10 mM in DMSO;IIJDFXNUWZTHIM-NRFANRHFSA-N;4′-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]- [1,1′-Biphenyl]-2-carboxylic acid;[1,1'-Biphenyl]-2-carboxylic acid, 4'-[[2,3-dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]-;Inhibitor,inhibit,HEK293T,F282,clash,SR1664,stereospecificity,PPAR,dependent,phosphorylation,SR-1664,S273,Peroxisome proliferator-activated receptors
- CBNumber
- CB72750678
- Molecular Formula
- C33H29N3O5
- Formula Weight
- 547.6
- MOL File
- 1338259-05-4.mol
4′-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]- [1,1′-Biphenyl]-2-carboxylic acid Property
- Boiling point:
- 828.8±65.0 °C(Predicted)
- Density
- 1.27±0.1 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- DMSO: soluble15mg/mL, clear
- pka
- 3.87±0.36(Predicted)
- form
- powder
- color
- white to beige
Safety
- Risk Statements
- 53
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- SML0636
- Product name
- SR1664
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $201
- Updated
- 2024/03/01
- Product number
- SML0636
- Product name
- SR1664
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $247.6
- Updated
- 2024/03/01
- Product number
- 11086
- Product name
- SR 1664
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $45
- Updated
- 2024/03/01
- Product number
- 11086
- Product name
- SR 1664
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $166
- Updated
- 2024/03/01
- Product number
- 11086
- Product name
- SR 1664
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $220
- Updated
- 2024/03/01
4′-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]- [1,1′-Biphenyl]-2-carboxylic acid Chemical Properties,Usage,Production
Uses
SR 1664 is a PPARγ non-agonist, which blocks Cdk5-mediated phosphorylation.
Definition
ChEBI: [1,1'-biphenyl]-2-carboxylic acid, 4'-[[2,3-dimethyl-5-[[[(1s)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1h-indol-1-yl]methyl]- is an indolecarboxamide.
Biological Activity
SR1664 is a non-agonist PPARγ ligand and an inhibitor of Cdk5-mediated PPARγ phosphorylation. It has strong antidiabetic activity in two murine models of diabetes without the side effects normally asociated with the thiazolidinedione (TZD) antidiabetic PPARγ agonists. The TZD antidiabetics such as rosiglitazone and pioglitazone are full PPARγ agonists, but recent data have suggested th at their separate activity, inhibition of the the obesity-linked PPARγ phosphorylation by Cdk5, is likely the more important activity for antidiabetic action. SR1664 has an IC50 of 80 nM in a competitive binding assay, blocked the Cdk5-mediated phosphorylation of PPARγ in vitro with IC50 between 20 and 200 nM and exhibited no PPARγ agonist activity.
4′-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]- [1,1′-Biphenyl]-2-carboxylic acid Preparation Products And Raw materials
Raw materials
Preparation Products
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