rxrα

Acitretin (Ro 10-1670) is a second-generation systemic retinoid used in the treatment of psoriasis.

K-8012 is a modulator of the N-terminally truncated RXRα and improves anticancer activities in an RXRα-dependent manner.

Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene. Fluorobexarotene  is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene.

Bexarotene (LGD1069) is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL).

1,3,5-Triisopropylbenzene is a benzene ring derivative commonly used in fuels, lubricants, and micellar expanders, and can be used as a potential retinoid X nuclear receptor alpha (RXRα) agonist (Activity Value=15µM).

β-Apo-13-carotenone is a naturally occurring β-apocarotenoid, and is a RXRα antagonist.

Magnolol (5,5'-Diallyl-2,2'-biphenyldiol) is a dual agonist of RXRα( EC50=10.4 μM) and PPARγ(EC50=17.7 μM). It blocks TNF-α-induced NF-KB activation.

β-Apo-13-carotenone D3 is the deuterium labeled β-Apo-13-carotenone. β-Apo-13-carotenone is an antagonist of RXRα.

UVI 3003 is a highly selective antagonist of the retinoid X receptor, inhibiting Xenopus and human RXRα in Cos7 cells with IC50 values of 0.22 μM and 0.24 μM, respectively.

K-80001 is a selective RXRα ligand and a COX-1 2 inhibitor, exhibiting IC50 values of 82.9μM for RXRα, 3.4μM for COX-1, and 1.2μM for COX-2, respectively [1].

AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; Kd= 2, 2, and 3 nM for RARα, β, and γ, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs; Kd= >10,000 nM for human RXRα, β, and γ receptors). This compound effectively reverses cellular morphology changes and growth suppression induced by RAR agonists such as all-trans-RA, 13-cis-RA, and 9-cis-RA in ECE16-1 human endometrial ectocervical epithelial cells, particularly when used at a 10-fold molar excess. Furthermore, AGN 193109 downregulates the expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, indicating inhibition of retinoid action, specifically when co-administered with TTNPB but not as a standalone treatment. In vivo studies demonstrate teratogenic effects, including cleft palate, frontonasal dysplasia, and eye malformations in mouse fetuses following a single oral dose of 1 mg kg.

6-Hydroxy Bexarotene, an oxidative metabolite of bexarotene, serves as a high-affinity ligand for retinoid X receptors (RXRs), specifically binding to RXRα, RXRβ, and RXRγ, as well as to the retinoic acid receptor α (RARα) with dissociation constants (Kds) of 3.46, 4.21, 4.83, and 8.17 μM, respectively. It demonstrates selective activation of RXRα, RXRβ, and RXRγ over RARα, RARβ, and RARγ in vitro, with half-maximal effective concentrations (EC50s) of 398, 356, 420, 4,414, 2,121, and 2,043 nM, respectively.

Drupanin, isolated from green propolis, selectively inhibits the AKR1C3 enzyme and shows promise for breast cancer research [1].

HX-600 is a synthetic agonist for the RXR-Nurr1 heterodimer complex. HX-600 prevents ischemia-induced neuronal damage.

GW0791 is a retinoid X receptor α (RXRα) agonist.

AGN194204 (IRX4204) is inactive against RAR and is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 has anti-inflammatory and antic

Elodeoidileon A acts as an agonist to RXRα, exhibiting a dissociation constant (Kd) of 5.85 μM when interacting with the RXRα-LBD protein. It enhances the expression of ATP Binding Cassette Transporter A1 (ABCA1). Furthermore, Elodeoidileon A holds potential in Alzheimer's disease research.

NBD-125 (B-12) is a berberine analogue. NBD-125 is an RXRα activator. The IC50 value of NBD-125 in KM12C cell is 31.10 μM [1].

22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22(S)-hydroxy Cholesterol also reduces fatty acid synthase (FAS) reporter activity through an LXR response element in the promoter region in COS-1 cells transfected with RXRα and LXRα and decreases the expression of MCP-1 and CCR2 in a mouse model of chronic ethanol consumption.[1] [2] Dietary supplementation of 22(S)-hydroxy cholesterol (30 mg/kg per day) leads to less body weight gain and lower liver triacylglycerol levels in rats when fed either a regular chow or high-fat diet as well as prevents an increase in plasma triacylglycerol levels resulting from a high-fat diet.[3]

CAY10771 is a dual agonist of farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor δ (PPARδ).1It activates FXR and PPARδ in reporter assays using HEK293T cells (EC50s = 0.94 and 1.5 μM, respectively) and is selective for these receptors over retinoic acid receptor α (RARα), retinoid X receptor α (RXRα), PPARα, PPARγ, and liver X receptor α (LXRα) at 10 μM. 1.Schierle, S., Neumann, S., Heitel, P., et al.Design and structural optimization of dual FXR/PPARδ activatorsJ. Med. Chem.63(15)8369-8379(2020)

Cecropin B acetate induces NF-κB activation and suppresses CYP3A29 by disrupting the association of the PXR retinoid X receptor alpha (RXR-α) complex with DNA sequences. Cecropin B acetate exhibits strong antimicrobial activity.

LG-100064 is an agonist of retinoid-X-receptor (RXR)(EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ)

BRF110 is a brain penetrant, potent and selective agonist of nuclear receptor-related 1 (Nurr1):Retinoid X receptor α (RXRα) heterodimer. BRF110 is a neuroprotective agent that prevents dopaminergic neuron demise and striatal dopaminergic denervation in vivo against PD-causing toxins. It induced dopamine biosynthesis in vivo. BRF110 chronic dosing does not induce dyskinesia in mice model.

MM 11253 is a RARγ antagonist with IC50 of 44nM.