Constitutive Androstane Receptor

The constitutive androstane receptor (CAR) is a member of the NR1I family of nuclear receptors, along with the pregnane X receptor and vitamin D receptor. The principal function of the constitutive androstane receptor is the sensing and clearance of foreign toxins.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
3683 CITCO
Selective CAR agonist
1225 TCPOBOP
Constitutive androstane receptor agonist

Antagonists

Cat No Product Name / Activity
5605 CINPA 1
Potent CAR antagonist
4096 Clotrimazole
Cytochrome P450 inhibitor. Also CAR inverse agonist
0670 PK 11195
CAR antagonist. Also peripheral benzodiazepine receptor antagonist
5188 S 07662
Inverse agonist of the constitutive androstane receptor (CAR)
2373 T 0901317
Potent LXR agonist; also CAR inverse agonist

The constitutive androstane receptor (CAR) is a member of the NR1I family of nuclear receptors, along with the pregnane X receptor and vitamin D receptor. CAR is involved in the sensing and clearance of foreign toxins through the upregulation of genes involved in xenobiotic clearance, including cytochrome P450, bilirubin, and multidrug transporters.

The name 'constitutive androstane receptor' refers to the unusual, constitutively active status of this receptor when not occupied by a ligand. Active constitutive androstane receptors bind to DNA as a heterodimer with RXRα, where they share common response elements with pregnane X receptors. The activity of these receptors is inhibited by the androstane metabolites, androstenol and androstanol, and can be induced by hypoxia inducible factor (HIF) activation. Recent research suggests that interactions between CAR and HIF lead to a reciprocal modulation of function.

In addition to its role in xenobiotic substance detection and clearance, the constitutive androstane receptor is also involved in the regulation of fatty acid β oxidation, gluconeogenesis and lipid metabolism. As a result, the constitutive androstane receptor is under investigation as a potential therapeutic target for metabolic disorders.

Literature for Constitutive Androstane Receptor

Nuclear Receptors

Nuclear Receptors Product Listing

A collection of over 150 products for key nuclear receptors, the listing includes research tools for the study of:

  • Androgen Receptors
  • Estrogen Receptors
  • Retinoic Acid Receptors
  • Retinoid X Receptors
  • Vitamin D Receptors

Constitutive Androstane Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
Constitutive Androstane Receptor Human NR1I3 NM_001077469 Q14994
Mouse Nr1i3 NM_009803 O35627
Rat Nr1i3 NM_001270838 Q9QUS1