gpr120 agonist 3

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

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 2 is a potent and selective GPR120 receptor agonist.

MOR agonist-3 (Compound 84) is a dual D3R/MOR antagonist with K i 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, an anti-NASH (Non-Alcoholic Steatohepatitis) agent, functions by activating FXR. It demonstrates anti-fibrogenic activity by inhibiting the expression of COL1A1, TGF-β1, α-SMA, and TIMP1. Additionally, it significantly mitigates liver steatosis and inflammation and enhances the liver fibrosis level [1].

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

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].

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.

GPR120 Agonist 1 is a selective GPR120 agonist. In GPR120 transfected HEK293 cells, GPR120 Agonist 1 displays good EC50 of 42 nM and 77 nM for human and mouse GPR120 (the calcium flux 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].

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.

5-HT2C agonist-3 ((+)-19) free base, a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM), 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. MRGPRX1 agonist 3 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.

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. THR-β agonist 3 has shown research potential for metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases.

5-HT2C agonist-3 ((+)-19), a selective 5-HT2C agonist (EC 50: 24 nM, Ki: 78 nM), exhibits antipsychotic-like activity by blocking amphetamine-induced hyperactivity [1].

TRβ agonist 3 (Compound 3) is a potent TRβ agonist that is a new potential TRβ-selective thyromimetics. In vitro investigation, TRβ agonist 3 reduces lipid accumulation in HepG2 and promote lipolysis [1].

SSTR4 agonist 3 is a potent compound that activates the SSTR4 receptor. The SSTR4 receptor is highly expressed in the hippocampus and neocortex, which are regions associated with memory, learning, and Alzheimer's disease pathology. SSTR4 agonists demonstrate strong efficacy in rodent models of pain, both acute and chronic, 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. RORγt agonist 3 induces Th17 cell differentiation, increases levels of pro-inflammatory cytokines and thus increases lymphocyte cytotoxicity. rorγt agonist 3 blocks the production of regulatory T cells and suppresses the immune response.

CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a competitive agonist for the CB1/CB2 receptors. It exhibits CB1/CB2 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 (Compound 2), a potent activator of toll-like receptor 7 (TLR7), plays a critical role in initiating immune responses, positioning it as a promising target for immunomodulator development.

GLP-1R agonist 3 is a thickened imidazole derivative compound that is a potent agonist of GLP-1R. GLP-1R agonist 3 has shown research potential in diabetes.

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].

RORγt Inverse agonist 3 is a potent, selective and orally active inverse agonist of RORγ(EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively).

APJ receptor agonist 3 is a highly effective and orally administerable agonist of the APJ receptor, demonstrating a potent EC50 value of 0.027 nM.

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). .

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.

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].

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