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CINPA1 

Cat. No.: HY-110249
Handling Instructions

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 IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function.

For research use only. We do not sell to patients.

CINPA1 Chemical Structure

CINPA1 Chemical Structure

CAS No. : 102636-74-8

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10 mM * 1 mL in DMSO USD 88 Ask For Quote & Lead Time
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Description

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 IC50 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].

Molecular Weight

395.49

Formula

C₂₃H₂₉N₃O₃

CAS No.

102636-74-8

SMILES

CCN(CC)CC(N1C2=CC(NC(OCC)=O)=CC=C2CCC3=C1C=CC=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

CINPA1CINPA 1CINPA-1OthersCARPXRInhibitorinhibitorinhibit

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