[CAS NO. 102636-74-8] CINPA1
PRODUCTS SPECIFICATIONS [102636-74-8]
DESCRIPTION [102636-74-8]
Overview
| MDL | MFCD00288296 |
|---|---|
| Molecular Weight | 395.49 |
| Molecular Formula | C23H29N3O3 |
| SMILES | CCN(CC)CC(N1C2=CC(NC(OCC)=O)=CC=C2CCC3=C1C=CC=C3)=O |
1 Publications Citing Use of MCE
Summary
CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC 50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function [1] .
IC50 & Target
IC50: ~70 nM (CAR) [1]
In Vitro
CINPA1 (1μM ; 24 hours) inhibits CAR-mediated transactivation without activating PXR in HepG2 cells
[1]
.
CINPA1 is a specific xenobiotic receptor inhibitor and has no cytotoxic effects up to 30 μM
[1]
.
CINPA1 inhibits CAR-mediated gene expression in primary human hepatocytes, where CAR is endogenously expressed
[1]
.
CINPA1 does not alter the protein levels or subcellular localization of CAR
[1]
.
CINPA1 increases corepressor and reduces coactivator interaction with the CAR ligand-binding domain in mammalian two-hybrid assays
[1]
.
CINPA1 disrupts CAR binding to the promoter regions of target genes in chromatin immunoprecipitation assays
[1]
.
CINPA1 efficiently inhibits CAR-LBD interaction with the coactivator peptide that suggesting that CINPA1 is a ligand of CAR
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 632.13 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5285 mL | 12.6425 mL | 25.2851 mL |
| 5 mM | 0.5057 mL | 2.5285 mL | 5.0570 mL |
| 10 mM | 0.2529 mL | 1.2643 mL | 2.5285 mL |