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Description: Potent CAR antagonist
Chemical Name: Ethyl [5-[(diethylamino)acetyl]-10,11-dihydro-5H-dibenz[b,f]azepin-3-yl]carbamate
Purity: ≥98% (HPLC)
Biological Activity for CINPA 1
CINPA 1 is a potent CAR antagonist (IC50 = 70 nM). Exhibits >90-fold selectivity for CAR over pregnane X receptor (PXR). Also selective over a panel of other nuclear receptors including FXR, LXR, PPARγ and RXR.
Compound Libraries for CINPA 1
CINPA 1 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for CINPA 1
| M. Wt | 395.49 |
| Formula | C23H29N3O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 102636-74-8 |
| PubChem ID | 969470 |
| InChI Key | AYQBYSPEGRYKFA-UHFFFAOYSA-N |
| Smiles | O=C(CN(CC)CC)N1C2=C(C=CC=C2)CCC3=C1C=C(NC(OCC)=O)C=C3 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CINPA 1
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.55 | 100 | |
| ethanol | 39.55 | 100 |
Preparing Stock Solutions for CINPA 1
The following data is based on the product molecular weight 395.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.53 mL | 12.64 mL | 25.29 mL |
| 5 mM | 0.51 mL | 2.53 mL | 5.06 mL |
| 10 mM | 0.25 mL | 1.26 mL | 2.53 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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Product Datasheets for CINPA 1
References for CINPA 1
References are publications that support the biological activity of the product.
Cherian et al (2015) CINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor. Mol.Pharmacol. 87 878 PMID: 25762023
If you know of a relevant reference for CINPA 1, please let us know.
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Keywords: CINPA 1, CINPA 1 supplier, CINPA1, CAR, constitutive, androstane, receptors, potent, antagonists, Constitutive, Androstane, Receptor, 5605, Tocris Bioscience
1 Citation for CINPA 1
Citations are publications that use Tocris products. Selected citations for CINPA 1 include:
Boussadia et al (2016) Lack of CAR impacts neuronal function and cerebrovascular integrity in vivo. Exp Neurol 283 39 PMID: 27240521
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Literature in this Area
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Nuclear Receptors Product Listing
A collection of over 150 products for key nuclear receptors, the listing includes research tools for the study of:
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