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CINPA1 

Cat. No.: HY-110249 Purity: 99.81%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 270 In-stock
Estimated Time of Arrival: December 31
50 mg USD 500 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (632.13 mM; Need ultrasonic)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.26 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.26 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.26 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.81%

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

CINPA1CINPA 1CINPA-1OthersCARPXRInhibitorinhibitorinhibit

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Product name:
CINPA1
Cat. No.:
HY-110249
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