RAR/RXR Agonist

BMS 753 is an isotype-selective retinoic acid receptor α (RARα) agonist, with a K_i of 2 nM.

AGN-195183 (IRX-5183) is a potent and selective agonist of RARα (K_d=3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ.

CD2314 is a potent and selective RARβ receptor agonist with a K_d of 195 nM in S91 melanoma cells.

Retinoic acid-d₅ is the the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC₅₀s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with K_d of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.

KCL-286 (C286) is an orally active and brain-penetrant retinoic acid receptor (RAR) β2 agonist (EC₅₀ = 1.9 nM). KCL-286 targets RARβ2 with good selectivity over RAR α (EC₅₀ = 26 nM) and RAR γ (EC₅₀ = 11 nM). KCL-286 activates RARβ2 in the injured neurons. KCL-286 induces axonal regeneration of both spinal and sensory nerves through the inhibitory environment of the CNS, modulates neuroinflammation and extracellular matrix molecules. KCL-286 can modulate the expression of CSPGs by neuronal secretion of decorin which promotes myelination and aids axonal growth. KCL-286 can be studied in research for area such as spinal cord injury and traumatic nerve injury.

BMS641 (BMS-209641) is a selective RARβ agonist. BMS641 has a higher affinity for RARβ (K_d, 2.5 nM) that is 100 times higher than that for RARα (K_d, 225 nM) or RARγ (K_d, 223 nM).

HX600 is a synthetic agonist for RXR (Retinoid X Receptor) heterodimer complex. HX600 prevents ischemia-induced neuronal damage. HX600 has orally bioactivity.

AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC₅₀ of 8.0.

BMS961 is a selective retinoic acid receptor-γ (RARγ) agonist. BMS961 shows anti-inflammatory activity.

AGN 194078 is a selective RARα agonist with a K_d and EC₅₀ of 3 and 112 nM, respectively.

MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the iNOS activity and reduces the expression of p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity.

WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist. WYC-209 induces apoptosis primarily via the caspase 3 pathway (IC₅₀=0.19 μM for inmalignant murine melanoma TRCs), and has long-term effects with little toxicity.

AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC₅₀ of 6.9.

9-cis-Retinoic acid-d₅ is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities.

ATRA-biotin (Biotin-ATRA-conjugate) is a biotin-conjugated ATRA. ATRA-biotin can be used to track ATRA in cells or a given tissue.

BMS270394 is a nuclear retinoic acid receptor (RAR-γ) agonist with the EC₅₀ values of 30 nM and 400 nM for humanRAR-γ and RAR-β, respectively.

Hydroxypinacolone retinoate (HPR) is a direct-binding agonist of retinoic acid receptor (RAR). Hydroxypinacolone retinoate has low irritation and high stability; when formulated into nanoparticles, its transdermal efficiency is enhanced, allowing it to penetrate deep into the dermis and achieve sustained release. When used in combination with Retinyl propionate, hydroxypinacolone retinoate promotes fibroblast proliferation and upregulates the gene expression of type IV collagen, CRBP-I and RARB. Hydroxypinacolone retinoate can be used in research related to skin wrinkles and skin aging.

Fluorobexarotene (compound 20) is a potent retinoid-X-receptor (RXR) agonist, with a K_i 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.

DC271 is a RAR agonist and synthetic retinoid that binds to the retinoid-binding site of cellular retinoic acid-binding protein II (CRBP-II). DC271 exhibits solvatochromic fluorescence properties: it produces intense blue-shifted emission in nonpolar environments and weak red-shifted emission in polar environments, and its severe fluorescence quenching in aqueous solutions can be reversed by embedding in the hydrophobic retinoid-binding protein pocket. DC271 enables direct detection of the binding between unlabeled compounds and related retinoid-binding proteins via fluorescence competition assays (Ex/Em = 355 nm/460 nm).

LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC₅₀s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer.