Date published: 2026-5-25

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CAR Activators

The chemical class of CAR activators encompasses a diverse spectrum of compounds designed to modulate the activity of the constitutive androstane receptor (CAR), a pivotal regulator involved in orchestrating drug metabolism and xenobiotic response pathways within the liver. This class of activators can be broadly classified into two categories: direct and indirect activators, each exerting their influence on CAR activity through distinctive mechanisms. Direct activators, exemplified by compounds like Phenobarbital, Rifampicin, CITCO, and TCPOBOP, engage with CAR by directly interacting with its ligand-binding domain. This interaction induces conformational changes within CAR, ultimately enhancing its transactivation capacity. The consequence of this direct activation is the upregulation of CAR-dependent genes, thereby influencing the pathways associated with drug metabolism and xenobiotic response. Notably, the well-established CAR activator, Phenobarbital, serves as a paradigmatic example, underscoring the significance of direct interactions in modulating CAR activity and regulating hepatic drug metabolism.On the other hand, indirect activators, represented by PBDE-47, 6-Formylindolo[3,2-b]carbazole, TCC, β-Naphthoflavone, Omeprazole, TCDD, Aroclor 1254, and Ciprofibrate, exert their influence on CAR activity through diverse signaling pathways. These compounds operate by modulating the aryl hydrocarbon receptor (AhR), pregnane X receptor (PXR), or peroxisome proliferator-activated receptor alpha (PPARα) pathways. The activation of these pathways, in turn, leads to the induction of CAR-responsive genes.

Items 1 to 10 of 12 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

TCPOBOP

76150-91-9sc-203291
25 mg
$209.00
4
(1)

TCPOBOP functions as a potent chemical activator, exhibiting unique interactions with target proteins through its electrophilic nature. Its reactivity is characterized by rapid acylation of nucleophilic sites, leading to distinct pathways in cellular signaling. The compound's steric properties enhance selectivity, allowing for precise modulation of enzymatic activity. Additionally, its stability under various conditions makes it a versatile tool for probing biochemical mechanisms and reaction kinetics.

Scoparone

120-08-1sc-202806
25 mg
$109.00
1
(1)

Scoparone acts as a selective chemical modulator, engaging in specific interactions with biomolecules through its unique structural features. Its ability to form stable complexes with target sites facilitates distinct regulatory pathways, influencing cellular processes. The compound's hydrophobic characteristics enhance membrane permeability, allowing for efficient distribution within biological systems. Furthermore, its reactivity profile showcases a balance between stability and reactivity, making it an intriguing subject for studying molecular dynamics.

PK 11195

85532-75-8sc-203199
sc-203199A
10 mg
50 mg
$88.00
$321.00
(1)

PK 11195 is a selective ligand that exhibits unique binding affinity for the translocator protein, influencing mitochondrial functions. Its distinct structural conformation allows for specific interactions that modulate cellular signaling pathways. The compound's lipophilic nature enhances its ability to traverse lipid membranes, promoting effective localization within cellular compartments. Additionally, its kinetic behavior reveals a nuanced balance between rapid association and slower dissociation, providing insights into receptor dynamics.

Rifampicin

13292-46-1sc-200910
sc-200910A
sc-200910B
sc-200910C
1 g
5 g
100 g
250 g
$97.00
$328.00
$676.00
$1467.00
6
(1)

Rifampicin, an antibiotic, is a direct activator of CAR, binding to its ligand-binding domain and inducing a conformational change that enhances CAR transactivation. This direct activation results in the upregulation of CAR-dependent genes, impacting drug metabolism and xenobiotic response pathways. Rifampicin's ability to activate CAR highlights its role in modulating hepatic drug metabolism and xenobiotic response elements.

CITCO

338404-52-7sc-202544
sc-202544A
5 mg
25 mg
$84.00
$312.00
4
(1)

CITCO (6-(4-chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oxime), a specific CAR agonist, directly activates CAR by binding to its ligand-binding domain, promoting CAR transactivation. This direct activation induces the expression of CAR-responsive genes, influencing drug metabolism and xenobiotic response pathways.

BDE No 47 solution

5436-43-1sc-233922
1 ml
$306.00
(0)

PBDE-47 (2,2',4,4'-Tetrabromodiphenyl ether), an environmental pollutant, indirectly activates CAR by influencing the aryl hydrocarbon receptor (AhR) pathway. PBDE-47 activates AhR, leading to the induction of CYP2B6, a CAR-responsive gene. This indirect activation highlights the crosstalk between AhR and CAR signaling pathways, suggesting a potential role for environmental pollutants in modulating CAR activity and hepatic drug metabolism.

6-Formylindolo[3,2-b]carbazole

172922-91-7sc-300019A
sc-300019
100 µg
5 mg
$105.00
$2185.00
5
(0)

6-Formylindolo[3,2-b]carbazole, an AhR agonist, indirectly activates CAR by modulating the AhR pathway. Activation of AhR by 6-Formylindolo[3,2-b]carbazole leads to the induction of CAR-responsive genes, impacting drug metabolism and xenobiotic response pathways. This indirect activation reveals the interconnectedness between AhR and CAR signaling and suggests a potential avenue for modulating CAR activity through the regulation of AhR signaling pathways.

Triclocarban

101-20-2sc-213106
100 mg
$260.00
1
(0)

TCC (3,3',4,4'-Tetrachlorocarbanilide), an antimicrobial agent, indirectly activates CAR by influencing the constitutive androstane receptor (CAR) pathway. TCC activates CAR, leading to the induction of CAR-responsive genes involved in drug metabolism and xenobiotic response. This indirect activation highlights the potential impact of antimicrobial agents on CAR activity and suggests a role for TCC in modulating hepatic drug metabolism through CAR-dependent mechanisms.

β-Naphthoflavone

6051-87-2sc-205597
sc-205597A
sc-205597B
sc-205597C
1 g
5 g
25 g
100 g
$33.00
$129.00
$599.00
$1647.00
2
(0)

β-Naphthoflavone, an AhR agonist, indirectly activates CAR by modulating the AhR pathway. Activation of AhR by β-Naphthoflavone leads to the induction of CAR-responsive genes, influencing drug metabolism and xenobiotic response pathways. This indirect activation underscores the interconnectedness between AhR and CAR signaling, providing insights into potential mechanisms for modulating CAR activity through the regulation of AhR signaling pathways.

Omeprazole

73590-58-6sc-202265
50 mg
$67.00
4
(1)

Omeprazole, a proton pump inhibitor, indirectly activates CAR by modulating the pregnane X receptor (PXR) pathway. Omeprazole activates PXR, leading to the induction of CAR-responsive genes involved in drug metabolism and xenobiotic response. This indirect activation highlights the crosstalk between PXR and CAR signaling pathways, suggesting a potential role for proton pump inhibitors in modulating CAR activity and hepatic drug metabolism.