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SML2468 Sigma-Aldrich

CINPA1

≥98%

Synonym: CAR Inhibitor not PXR Activator 1, Ethyl 5-(2-(diethylamino)acetyl)-10,11-dihydro-5H-dibenzo[b,f]azepin-3-ylcarbamate, [5-[(Diethylamino)acetyl]-10,11-dihydro-5H-dibenz[b,f]azepin-3-yl]carbamic acid ethyl ester

  • CAS Number 102636-74-8

  • Empirical Formula (Hill Notation) C23H29N3O3

  • Molecular Weight 395.49

  •  MDL number MFCD00288296

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, CI-CZ, Cell Biology
assay   ≥98%
form   powder
color   white to beige
solubility   DMSO: 2 mg/mL, clear
storage temp.   −20°C
SMILES string   O=C(CN(CC)CC)N1C2=C(C=CC=C2)CCC3=C1C=C(NC(OCC)=O)C=C3

Description

Biochem/physiol Actions

CINPA1 is a ligand-binding domain (LBD)-targeting constitutive androstane receptor (CAR) inhibitor that prevents CAR recruitment to promoter regions of regulated genes (by >85%; 1 μM CINPA1 against 0.1 μM CITCO-induced CAR recruitment to CYP2B6 or CYP3A4 promoters; human hepatocytes) by altering CAR-coregulator interactions. CINPA1 inhibits CAR-mediated transcription in a potent (IC50 = 70 nM; HepG2-hCAR1 CYP2B6-luc reporter cells) and selective manner with only weak PXR antagonist potency (68% inhibition by 18 μM CINPA1 against 5 μM rifampicin; HepG2-PXR reporter cells) and no cytotoxicity or agonist/antagonist activity toward FXR, GR, LXRα/β, PPARγ, RXRα/β, VDR.

Safety & Documentation

Safety Information

WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles
Peer-Reviewed Papers
15

References

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