ahr agonist 3

AHR agonist 3 is an agent with therapeutic activity.

GPR35 agonist 3 is a synthetic GPR35 agonist with an EC50 value of 1.4 μg in the β-arrestin recruitment assay.GPR35 agonist 3 is used in the study of cancer, type 2 diabetes, and cardiovascular disease.

TLR7 8 agonist 3 is a potent activator of TLR7 and TLR8.

GLP-1 receptor agonist 3 is a GLP-1 receptor agonist,Example 4A-1, has EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.

TGR5 Receptor Agonist 3 is a G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist soft drug compound that decreases gallbladder filling, exhibits good gallbladder safety, and is able to act on hTGR5 (EC50: 16.4 nM) and mTGR5 (EC50: 209 nM).

PPARγ agonist 3, also known as Compound 18a, is a potent and selective agonist of PPARγ. This compound does not exhibit cytotoxicity towards both non-resistant and resistant cells. Notably, PPARγ agonist 3 demonstrates antitumor efficacy exclusively when co-administered with Imatinib [1].

5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM. It also demonstrates a remarkable 124-fold selectivity over its structurally analogous 5-HT2C receptor [1].

Compound CMC23, an FPR2 agonist, mitigates lactate dehydrogenase release in LPS-stimulated cultures and reduces pro-inflammatory IL-1β and IL-6 levels. It also attenuates phosphor-STAT3 levels through the STAT3/SOCS3 signaling pathway [1].

STING agonist-3 trihydrochloride is a selective and non-nucleotide agonist of small-molecule STING(pEC50 and pEC50 of 7.5 and 9.5, respectively), has durable anti-tumor effect and tremendous potential to improve treatment of cancer.

AhR agonist 2 (Compound 12a) is a highly potent agonist of the aryl hydrocarbon receptor (AhR) with an EC50 of 0.03 nM, rapidly inducing nuclear AhR enrichment and initiating transcription of downstream genes to promote skin barrier repair. AhR agonist 2 shows promising potential for psoriasis research [1].

THR-β agonist 3 is a potent agonist of THR-β with demonstrated research potential for metabolic diseases, including obesity, hyperlipidemia, hypercholesterolemia, diabetes, steatosis, non-alcoholic steatohepatitis (NASH), and atherosclerosis.

5-HT2C agonist-3 ((+)-19) free base is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM) that exhibits antipsychotic drug-like activity and inhibits Amphetamine-induced hyperactivity [1].

MRGPRX1 agonist 3 (compound 1f) is a potent positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MRGPRX1) with an EC50 of 0.22 μM, and it can be used for neuropathic pain research[1].

GP 2A is a selective agonist of CB2 receptor.

Wnt/β-catenin agonist 3 is a Wnt/beta-catenin agonist.

MOR agonist-3 (Compound 84) is a dual D3R MOR antagonist with Ki values of 382 nM and 55.2 nM, respectively. It shows promise for analgesia via partial agonism at MORs and may mitigate opioid abuse via D3R antagonism. This compound is utilized in research pertaining to inflammation and neuropathic pain [1].

FXR agonist 3 is an anti-NASH compound with antifibrotic and anti-fibrotic activity, inhibiting the expression of COL1A1, TGF-β1, α-SMA, and TIMP1, with an IC50 value of 8.19 μmol L for COL1A1. FXR agonist 3 ameliorates CDAHFD and BDL-induced liver injury in vivo by activating FXR.

TLR7 agonist 3 is a Toll-like receptor 7 (TLR7) agonist that has anticancer activity and is used in the study of diseases of the immune system.

TRβ agonist 3 (Compound 3) is a potent TRβ agonist and a potential TRβ-selective thyromimetic. In vitro studies show that TRβ agonist 3 reduces lipid accumulation in HepG2 cells and promotes lipolysis [1].

CB1 2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, acts as a competitive agonist for the CB1 and CB2 receptors, exhibiting agonistic activity by binding to the human CB1 and CB2 receptors with Ki values of 5.9 nM and 3.5 nM, respectively [1].

SSTR4 agonist 3 is a potent compound that activates the SSTR4 receptor, which is highly expressed in the hippocampus and neocortex—regions associated with memory, learning, and Alzheimer's disease pathology. SSTR4 agonists demonstrate strong efficacy in rodent models of both acute and chronic pain by reducing peripheral nociception and inflammation. Considering its potential application in pain research, SSTR4 agonist 3 is of interest [1].

RORγt agonist 3 is a potent agonist of RORγt that induces Th17 cell differentiation, increases levels of pro-inflammatory cytokines, and enhances lymphocyte cytotoxicity. Moreover, [it] blocks the production of regulatory T cells and suppresses the immune response.

AHR agonist 4 (compound 24e), as an Aryl hydrocarbon receptor (AHR) agonist, modulates the immune equilibrium between Th17/22 and Treg cells. It is a lead compound under investigation for anti-psoriasis drugs and demonstrates efficacy in mitigating imiquimod (IMQ)-induced psoriasis-like skin lesions [1].

5-HT2C agonist-3 ((+)-19), a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM), exhibits antipsychotic-like activity by blocking amphetamine-induced hyperactivity [1].

GLP-1R agonist 3 is a potent imidazole derivative and GLP-1R agonist with demonstrated research potential in diabetes. [Thickened]

RXFP1 receptor agonist-3 (Example 223) is an RXFP1 receptor agonist that inhibits cyclic AMP (cAMP) production in HEK293 cells stably expressing human RXFP1, with an EC50 of 2 nM [1].

LXRβ agonist-3 is a potent and selective LXRβ (liver X receptor β) agonist (EC50: 0.095 μM). LXRβ agonist-3 effectively inhibits U87EGFRvIII cells (IC50: 3.75 μM). .

Compound 8, a cholic acid derivative, functions as a selective TGR5 agonist and exhibits an EC50 value of 5 μM [1].

Compound 20, identified as μ opioid receptor agonist 3, is a potent µOR agonist that exhibits an EC50 value of 0.87 nM. It holds promise for research into pain management and neuropsychiatric disorders [1].

GPR120 Agonist 3 (GPR120-IN-1) is a selective agonist of Gpr120 ( logEC50: -7.62).

RORγt Inverse Agonist 3 is a potent, selective, and orally active inverse agonist of RORγ with EC50 values of 0.22 μM for hRORγ and 0.15 μM for RORγt (human IL-17 cells), respectively.

APJ receptor agonist 3 is a highly effective, orally administrable APJ receptor agonist, with a potent EC50 value of 0.027 nM.

STING agonist-3 is a selective and non-nucleotide small-molecule STING agonist(pEC50 and pIC50 of 7.5 and 9.5, respectively), has durable anti-tumor effect and tremendous potential to improve treatment of cancer.

Compound 26, a GPR55 agonist, exhibits potent activity with EC50 values of 0.239 nM for hGPR55 and 1.76 nM for rGPR55. It also induces β-arrestin recruitment to human GPR55 with an EC50 of 6.2 nM [1].

CB2R agonist 3, a potent activator of cannabinoid receptor 2 (CB2R), exhibits an EC50 value of 0.37μM, indicative of its significant role in the immune system [1].

MeBIO is an agonist of aryl hydrocarbon receptor, with IC50 of 44 and 55 μM for GSK-3 and CDK1/CyclinB, respectively. MeBIO does not affect GSK-3β.

ITE is a potent endogenous agonist of the aryl hydrocarbon receptor (AhR) (Ki: 3 nM) with immunosuppressive activity.

Flavipin, an aryl hydrocarbon receptor (Ahr) agonist, activates Ahr downstream gene expression in mouse CD4+ T cells and CD11b+ macrophages. This compound disrupts the stabilizing effect of Arid5a on the newly identified target mRNA, Il23a 3′UTR. Additionally, Flavipin demonstrates significant antioxidant properties, evidenced by its DPPH free radical scavenging capability with an IC50 value of 7.2 μM, and exhibits potent α-glucosidase inhibitory activity with an IC50 value of 33.8 μM.

Potassium 1H-indol-3-yl sulfate (Potassium 3-indoxyl sulfate) is an agonist for the human Aryl Hydrocarbon Receptor (AhR), a key regulator of immune-inflammatory conditions. A metabolite of tryptophan derived from dietary protein, it is produced by intestinal bacteria and metabolized in the liver. In chronic kidney disease patients with impaired renal function, it accumulates in serum as a uremic toxin, inducing oxidative stress and accelerating disease progression. At 250 μM, it activates NF-Κb, promoting TGF-β1 and Smad3 expression in rat proximal tubular cells, which is associated with profibrotic activity.

Methacholine bromide (Acetyl-β-methylcholine bromide) is a potent muscarinic-3 (M3) agonist that specifically acts on acetylcholine receptors located on smooth muscle, inducing bronchoconstriction and narrowing of the airways. Its high sensitivity in identifying bronchial hyperresponsiveness (BHR), a hallmark of asthma, makes it useful in the assessment of airway hyperresponsiveness (AHR) as a diagnostic tool for individuals exhibiting asthma-like symptoms with normal resting expiratory flow rates [1] [2] [3] [4].

Indolokine A4, a catabolite of indole-3-pyruvate (I3P), is a potent AhR agonist.