receptor agonist

β2AR/M-receptor agonist-2 is a dual-function compound acting as a muscarinic antagonist and β2 adrenoceptor agonist (MABA). It demonstrates significant activity towards the β2 adrenoceptor with an EC50 of 3.7 nM and exhibits affinity for the human cloned M3 receptor with a Ki of 0.73 nM. This potent bronchodilator holds potential for research in chronic obstructive pulmonary disease (COPD) treatment.

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.

GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist with an EC50 of 64.5 nM, and is utilized in diabetes treatment research.

GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.

Glucocorticoid receptor agonist is an effective glucocorticoid receptor agonist.

TGR5 is a potent TGR5(GPCR19) agonist.

5-HT2A receptor agonist-6 (compound 47) is a selective agonist of the 5-HT2A receptor with a pEC50 value of 6.58.

APJ receptor agonist 10 (Compound I choline salt) modulates the activity of the APJ receptor, making it useful for pulmonary hypertension research. Compared to its free form, this compound exhibits improved bioavailability.

CB2 receptor agonist 9 (Compound 33) is an orally active agonist of cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. It inhibits the expression of TNF-α, IL-1β, and IL-6, demonstrating anti-inflammatory activity in a DSS-induced acute colitis model in mice.

CB2 receptor agonist 8 (Compound 17) is an agonist of the cannabinoid receptor 2 (CB2 receptor). It shows cytotoxicity in U87, RPMI 8226, HL-60, and L929 cells with IC50 values of 91.03, 16.29, 23.51, and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expression of pro-apoptotic genes BAX, BAD, BIM, and the tumor suppressor gene p53, and induces apoptosis in U87 cells. Additionally, it inhibits the migration of U87 cells.

5-HT2A receptor agonist-5 (compound I-3) is a potent 5-HT2A agonist with a Ki value of 0.017 µM and exhibits antidepressant activity.

EP4 receptor agonist 3 is an activator of the EP4 receptor and is useful for research in the DSS-induced colitis mouse model.

GLP-1 receptor agonist 15 (Example 4) is a GLP receptor agonist with an EC50 of 0.74 nM. It exhibits an IC50 of 10.1 μM against the hERG potassium ion channel. This compound is applicable for research in the diabetes field.

Opioid receptor agonist1 (Compound 2638-28) is an orally active opioid receptor agonist that shows strong affinity for MOR, DOR, and KOR, with Ki values of 5, 24, and 212 nM, respectively. It exhibits analgesic activity in both the mouse warm water tail-flick model and the acetic acid writhing model.

5-HT2A receptor agonist-7 (517) functions as a modulator of the 5-HT2A receptor, with an EC50 value of less than 100 nM.

GLP-1 receptor agonist 17-d3 (Compound 701) is the deuterated form of GLP-1R agonist 17, which acts as a GLP-1 receptor agonist and is applicable in cardiovascular and metabolic disease research.

5-HT2A receptor agonist-8 (compound 8) is a potent 5-HT2A receptor agonist with an EC50 of 0.6784 nM. It is suitable for research related to depression and bipolar disorder.

5-HT2A receptor agonist-9 is a β-arrestin-biased agonist of the 5-HT2A receptor. It may be utilized in research related to neurological conditions such as depression and psychedelia.

Orexin 2 Receptor Agonist 3 is an orally active and brain-penetrant agonist of the orexin receptor 2 (OX2) with an EC50 value of 2.5 nM. This compound increases wakefulness in both orexin/ataxin-3 NT1 mouse models and healthy Beagle dogs. It is applicable for research related to narcolepsy.

RXFP1 receptor agonist-9 is a potent RXFP1 agonist with an EC50 value of 2.5 μM and a Ymax of 65%. This compound exhibits significant microsomal stability, desirable pharmacokinetic properties, and pharmacodynamic activity. RXFP1 receptor agonist-9 is useful in the study of heart failure.

RXFP1 receptor agonist-10 (Compound 188) is an RXFP1 receptor agonist with an EC50 of 0.5 nM. It is useful for research into heart failure.

5-HT2A receptor agonist-10 (Compound (R)-I-121.HCl) acts as a 5-HT2A receptor agonist with IC50 values of 2192.39 nM for h5-HT2A and 33.57 nM for h5-HT1A. It is applicable in research related to psychiatric disorders, mental illnesses, and central nervous system diseases.

Adenosine receptor agonist2 (Compound 10) is an agonist of the adenosine A2B receptor (A2BR) with an EC50 of 0.38 nM. It significantly inhibits the accumulation of cAMP and calcium ions. Adenosine receptor agonist2 is applicable in cardiovascular protection studies.

THRβ receptor agonist-2 (Example 7-4) is a THRβ receptor agonist that can be utilized in research related to liver diseases or cardiometabolic disorders.