Wnt/β-catenin agonist 3

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

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.

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

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

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].

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.

GPR88 agonist 3 (compound 20), exhibiting an EC50 of 204 nM, functions as an agonist for GPR88. It is applicable in the research of psychiatric and neurodegenerative disorders [1].

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].

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].

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].

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.

Wnt/β-catenin agonist 4 is an agonist of Wnt that activates Wnt/β-catenin signaling and directs signaling.

GP 2A is a selective agonist of CB2 receptor.

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.

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.

Wnt β-catenin-IN-2 (Compound 3235-0367) serves as an inhibitor of the Wnt β-catenin signaling pathway, exhibiting IC50 and KD values of 7.1 and 2.5 μM, respectively. It is applicable in cancer research [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].

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].

β-Catenin modulator-3 (compound IIa-112), an oxazole and thiazole-based chemical entity, serves as a potent and selective modulator of β-Catenin [1].

hCA Wnt β-catenin-IN-1 (Compd 15) is an inhibitor selectively targeting hCA isoforms II, IX, and XII, with K i values of 33.6, 24.1, and 6.8 nM, respectively. It also attenuates P-gp activity, disrupts the Wnt β-catenin signaling pathway, and compromises the viability of cancer cells, specifically against the NCI ADR-RES DOX-resistant cell line [1].

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

Wnt/β-catenin agonist 1 is an agonist of Wnt/β-catenin signalling pathway(EC50 of 0.27 μM).

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].

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.

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].

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].

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.

Muscarinic agonist 3 (compound 45) is a muscarinic mAChR M1 M2 M4 agonist with EC50 values of 3.2 nM, 32 nM, and 1.7 nM, respectively [1].

Wnt β-catenin-IN-3 (compound 17), a Wnt β-catenin inhibitor, exhibits low micromolar GI 50 s across different cancer cell lines. It induces G2 M cell cycle arrest through the activation of the p53-p21 pathway and promotes both intrinsic and extrinsic apoptotic death in colon cancer cells [1].

Compound 9a (β2AR agonist 3) is a β2-adrenergic receptor (β2AR) agonist used in type 2 diabetes research [1].

β-catenin-IN-3 is a selective and potent β-catenin inhibitor (KD: 54.96 nM) that targets a cryptic regulatory site of β-catenin and significantly reduces the viability of β-catenin-driven cancer cells.

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].

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].

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].

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.

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). .

Glucocorticoid Receptor Agonist-3 Ala-Ala-Mal (Compound Preparation 8) is a conjugate of an anti-human TNFα antibody and a glucocorticoid receptor agonist (GC). It is utilized in researching autoimmune and inflammatory diseases [1].

Wnt β-catenin agonist 2 activates Wnt β-catenin signaling and is an effective Wnt agonist. Wnt β-catenin agonist 2 can be used in the study of diseases related to signal transduction and is closely related to cancer invasion and metastasis.

Wnt pathway inhibitor 3 is a potent AC1 inhibitor (IC50: 45 nM) with antiproliferative activity, suitable for studies to ameliorate osteoarthritis in a mouse model of experimental osteoarthritis.

Compound 44, identified as an M1 M4 muscarinic agonist, exhibits potent activity with EC50 values of 31 nM at M1 and 9.3 nM at M4 mAChRs, respectively [1].

Compound 15A, also known as A3AR agonist 3, acts as an agonist for the A3 adenosine receptor (A3AR), exhibiting K_i and EC_50 values of 2.27 nM and 0.20 nM for hA3 and cAMP, respectively. This compound is utilized in neuroinflammation research [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].

AHR agonist 3 is an agent with therapeutic activity.