selective,?retinoid

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

AGN 205327 is a potent synthetic agonist of retinoic acid receptors (RARs), with EC50 values of 3766 nM for RARα, 734 nM for RARβ, and 32 nM for RARγ, and AGN 205327 demonstrates no inhibitory activity against retinoid X receptors (RXRs), thereby exhibiting selective receptor subtype targeting that makes AGN 205327 an important tool for probing retinoid signaling pathways and investigating therapeutic applications of RAR activation.

AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ. IC₅₀ value: 3 nM (Kd); 200 nM (EC80, RAR Trans.) Target: RARα agonist Compound 4(AGN-195183) inhibited the growt

CD3254 is a selective and potent retinoid X receptor-like (RXR) agonist that inhibits neuronal cell death with OGD/reoxygenation.

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.

LG100268 is a potent, selective, and orally active retinoid X receptor (RXR) agonist that agonizes RXR-α, RXR-β, and RXR-γ at the nanomolar level, selectively exceeding the RAR by three orders of magnitude.LG100268 is capable of inducing transcriptional activation in adipocytes; affecting the RXRs and their chaperone receptor, Foxl2/Dmrt1, to induce flounder masculinization in juvenile flounder; inhibits keratin 17 expression in nigrostriatal epithelial cells; and increases PD-L1 expression in HER2 or triple-negative breast cancer.

RXR agonist 2 (Compound 22) is a highly selective agonist of the retinoid X receptor (RXR) with an EC50 of 0.039 μM. It shows potential for use in research on metabolic syndrome and Alzheimer's disease.

RXR antagonist 6 (Compound 34) is a selective partial antagonist of the retinoid X receptor (RXR). It exhibits no agonistic activity on human RXRα/β/γ subtypes, but it effectively inhibits receptor activation induced by full RXR agonists such as Bezafibrate, with an IC₅₀ value of 2.7 μM. Additionally, RXR antagonist 6 can enhance PMA-induced differentiation of THP-1 cells and is applicable in research related to cancer, metabolic disorders, and neurological diseases, including lymphoma.

BMS453 (BMS-189453), a synthetic retinoid, is a potent and selective agonist of RARβ and a potent testicular toxin. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.

TBTC is a selective agonist of retinoid X receptor α that acts by improving behavioral deficit in Alzheimer's disease model mice.

Latanoprost (Xalatan) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.

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)

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.

CU239 is a selective non-retinoid inhibitor of RPE65 which suppresses visual cycle and prevents retinal degeneration.

Trifarotene (CD5789) is a potent and selective RARγ agonist, exhibiting 65-fold and 16-fold selectivity for RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM).

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.

(all-E)-UAB30 (UAB30) is a selective agonist for the retinoid X receptor (RXR). It exhibits antiproliferative activity against MyLa, HuT 78, and HH cell lines, with IC₅₀ values of 34.7, 5.1, and 22.4 μM, respectively.

9-cis-13,14-Dihydroretinoic acid (9CDHRA) is a selective retinoid X receptor (RXR) agonist with a Kd of 90 nM. It can ameliorate memory deficits caused by impaired RXR signaling in vivo. This compound shows potential for research in the fields of neuroscience and metabolic diseases.

Bigelovin is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.It is also known as a potent cytotoxic sesquiterpene lactone from Inula sp.