A CAR antagonist
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CINPA1

Item No. 29110

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[5-[(diethylamino)acetyl]-10,11-dihydro-5H-dibenz[b,f]azepin-3-yl]-carbamic acid, ethyl ester
CAS Number
102636-74-8
Molecular Formula
C23H29N3O3
Formula Weight
395.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mMEthanol: 100 mM
SMILES
O=C(CN(CC)CC)N1C(C=C(NC(OCC)=O)C=C2)=C2CCC3=C1C=CC=C3
InChi Code
InChI=1S/C23H29N3O3/c1-4-25(5-2)16-22(27)26-20-10-8-7-9-17(20)11-12-18-13-14-19(15-21(18)26)24-23(28)29-6-3/h7-10,13-15H,4-6,11-12,16H2,1-3H3,(H,24,28)
InChi Key
AYQBYSPEGRYKFA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $103

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    10 mg

    $169

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    Product Description

    CINPA1 is a constitutive androstane receptor (CAR) antagonist (IC50 = 70 nM in a reporter assay).1 It is selective for CAR over the nuclear receptors GR, FXR, LXRα, LXRβ, PPARγ, RXRα, and RXRβ at 18 μM, but also antagonizes the human pregnane X receptor (PXR; IC50 = 6.6 μM). CINPA1 (0.3-5 μM) inhibits CAR transactivation of CYP2B6 induced by CITCO (Item No. 16027) in primary human hepatocytes.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cherian, M.T., Lin, W., Wu, J., et al. CINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor. Mol. Pharmacol. 87(5), 878-889 (2015).