RAR/RXR Agonist

TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC₅₀s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.

Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC₅₀s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC₅₀ >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma.

AM580 is a selective RARα agonist with IC₅₀ and EC₅₀ of 8 nM and 0.36 nM, respectively.

Tamibarotene is an orally active retinoic acid receptor α (RARα) agonist, showing high selectivity over RARγ.

Trifarotene-d₄ (Cd₅789-d₄) is the deuterium labeled Trifarotene (HY-100256). Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ～65-fold and ～16-fold selectivitiy for the RARγ (EC₅₀=7.7 nM) over RARα (EC₅₀=500 nM) and RARβ (EC₅₀=125 nM), respectively.

Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC₅₀s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity.

CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.

Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.

Acitretin (Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis. Acitretin also can be used for the research of Alzheimer’s disease.

Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Retinoic acid (Vitamin A acid) (GMP) is Retinoic acid (HY-14649) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Retinoic acid is an agonist of RAR nuclear receptors.

SR11237 (BMS-649) GMP is SR11237 (HY-107413) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SR11237 is a RXR activator and lipid metabolism regulator that promotes the differentiation of induced neural stem cells into dopaminergic (TH-positive) neurons. SR11237 induces transcriptional regulation of lipogenic genes and cholesterol transporters, increases glycosaminoglycan release, and elevates total cellular triglyceride levels. SR11237 promotes heterodimerization of RXR with Nurr1, thereby enhancing tyrosine hydroxylase expression and facilitating dopamine release. SR11237 produces a synergistic effect when used in combination with bFGF/EGF. SR11237 is mainly used in studies related to osteoarthritis and Parkinson's disease.

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.

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.

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.

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.

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.