constitutive androstane receptor

Epsilon-momfluorothrin (Momfluorothrin, (Z,1R,3R)-), a type I synthetic pyrethroid insecticide, exerts its insecticidal properties and triggers activation of the constitutive androstane receptor (CAR). Notably, its administration in rats has been observed to induce the development of hepatocellular tumors.

Meclizine, also known as Meclozine, is a piperazine class H1 antagonist with antihistamine properties that inhibits the interaction of histamine at H1 receptors reversibly. It serves as an effective anti-motion sickness agent, able to cross the blood-brain barrier. Additionally, Meclizine acts as an agonist ligand for the mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR, making it useful in research on polyQ toxicity disorders, including Huntington's disease.

CINPA1 (CINPA 1) is a selective inhibitor of constitutive androstane receptor (CAR) with an IC50 of 70 nM for CAR-mediated transcription. CINPA1 can be used in studies about CAR function.

CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors. CITCO is an imidazothiazole derivative and it also is a selective Constitutive androstane receptor (CAR) agonist.

TCPOBOP, a constitutive androstane receptor agonist, induces robust hepatocyte proliferation and hepatomegaly while decreasing Fas-induced murine liver injury by altering Bcl-2 proteins.

DL5050 is a selective agonist for the human constitutive androstane receptor (hCAR). This compound demonstrates superior affinity and selectivity for hCAR by inducing expression of CYP2B6 (the target of hCAR) at the mRNA and protein levels, rather than CYP3A4 (the target of the human pregnane X receptor, hPXR). As a selective hCAR agonist, DL5050 not only serves as a crucial tool molecule for studying hCAR's biological function but also holds potential as a lead compound for the development of therapeutic applications targeting hCAR.

MI-883 is an orally active Constitutive Androstane Receptor (CAR, EC50=73 nM) agonist and a Pregnane X Receptor (PXR, IC50=0.1 μM) antagonist. It enhances CAR LBD assembly (EC50=0.38 µM) and activates the CAR3 variant (EC50=0.074 µM), inducing CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. Additionally, MI-883 inhibits the basal activity of PXR (IC50=2.03 µM) and reduces CYP3A4 mRNA expression in transiently transfected HepG2 cells. It also regulates cholesterol metabolism and bile acid excretion, improving hypercholesterolemia in mouse models.

5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. It inhibits the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). By binding to CAR and promoting its dissociation from coactivator proteins, 5α-Androstan-3α-ol negatively regulates CAR's activity. This compound is useful for studying hormone metabolism and drug detoxification mechanisms mediated by nuclear receptors.

S07662 is an inverse agonist of human CAR (IC50=0.7 μM), promoting NCoR recruitment and inhibiting proteasomal degradation of proteins, suitable for cancer research.

1. (±)-Praeruptorin A could exhibit its anti-osteoclastogenic activity by inhibiting p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca(2+) oscillation 2. Praeruptorin A has the potential to inhibit migration/fusion of preosteoclasts in vitro and bone erosion in vivo by targeting calmodulin and inhibiting the Ca(2+)/calmodulin-CaMKIV-CREB-NFATc1 and/or Ca(2+)/calmodulin-calcineurin-NFATc1 signaling axis. 3. Praeruptorin A and praeruptorin C can significantly upregulate multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.

Z-CITCO acts as an agonist for the constitutive androstane receptor (CAR; with an EC50 of 3.9 µM in human receptor reporter assays) and is the cis isomer of the CAR agonist CITCO.

(±)-Praeruptorin A (Standard) is a reference standard for research and analysis in studies involving (±)-Praeruptorin A. 1. (±)-Praeruptorin A could exhibit its anti-osteoclastogenic activity by inhibiting p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca(2+) oscillation 2. Praeruptorin A has the potential to inhibit migration/fusion of preosteoclasts in vitro and bone erosion in vivo by targeting calmodulin and inhibiting the Ca(2+)/calmodulin-CaMKIV-CREB-NFATc1 and/or Ca(2+)/calmodulin-calcineurin-NFATc1 signaling axis. 3. Praeruptorin A and praeruptorin C can significantly upregulate multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.