apj receptor agonist 4

APJ Receptor Agonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models and has shown an acceptable safety profile in preclinical toxicology studies. This compound effectively improves cardiac function, making it valuable for research into HF disease.

CB2 receptor agonist 2 (ZINC72105556) is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor, Ki = 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.

Dopamine D2 receptor agonist-2 (Dopamine D2 Receptor) is a ligand targeting the dopamine D2 receptor.

Protease-Activated Receptor-4 diTFA,2454 is the proteinase-activated receptor-4 (PAR4)agonist

Protease-Activated Receptor-1, PAR-1 Agonist acetate is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist acetate corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].

GLP-1 receptor agonist 9 citrate is an agonist of GLP-1.

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.

Glucocorticoid receptor agonist-1, a potent glucocorticoid receptor agonist, has an IC50 of 2.8 nM[1].

Adenosine receptor antagonist 4 is an adenosine receptor antagonist.

GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist.

C3a Receptor Agonist (C3a receptor agonist 1) binds the G protein-coupled C3a receptors (C3aRs) in the immune system complement pathway. Activation of C3aR prevents neutrophils from being mobilized in a model of intestinal ischemia-reperfusion injury. C3aRs are expressed on neural progenitor cells and immature neurons in adult mice. C3a stimulates differentiation of neural progenitor cells in vitro.

1H-Benzimidazole-6-carboxylic acid is a GLP-1 receptor agonist.

Orexin 2 Receptor Agonist (OX2R) is an effective (EC50: 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio: 70) agonist.

PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)), is a selective activator of the proteinase-activated receptor-4 (PAR-4) that does not affect PAR-1 or PAR-2, and its activity can be inhibited by a PAR-4 antagonist.

S1p receptor agonist 1 (S1p-receptor-agonist-1) is an S1P receptor agonist.

APJ Receptor Agonist 8 (compound 99) acts as an agonist for the APJ receptor and enhances load-independent cardiac contractility in isolated perfused rat hearts [1].

RORγt agonist 4 (compound 14) acts as a potent and selective agonist for RORγt, significantly boosting metabolic stability. It also enhances the condition in mouse tumor models, specifically B16F10 melanoma and LLC lung adenocarcinoma [1].

Protease-Activated Receptor-1 (PAR-1) Agonist TFA is a selective peptide that acts as an agonist for the proteinase-activated receptor-1 (PAR-1). Corresponding to the tethered ligand of PAR-1, this compound mimics the actions of thrombin through the PAR-1 receptor[1][2].

RXFP1 receptor agonist-4 (Example 268) is a potent RXFP1 receptor agonist, shown to effectively suppress cAMP production in HEK293 cells stably expressing the human RXFP1 receptor, with an effective concentration (EC50) of 4.9 nM [1].

TLR7 8 agonist 4 (compound 41) is a potent TLR7 8 agonist with demonstrated anti-cancer activity [1].

Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88), a glucocorticosteroid and glucocorticoid receptor agonist, can be conjugated with Adalimumab to formulate an ADC [1].

Glucocorticoid receptor agonist-2 (compound 21), a glucocorticoid receptor agonist with an IC50 value of 6.6 nM, serves as an active reference for ABBV-3373 [1] and is instrumental in the synthesis of anti-inflammatory ADC molecules.

Estrogen Receptor Antagonist 4 is a potent inhibitor of the estrogen receptor (ER), crucial for regulating cell growth, differentiation, and apoptosis. This compound holds promise for cancer research[1].

Thrombin receptor agonist peptide (TRAP-14) is a 14-amino acid peptide agonist of the α-thrombin receptor. It induces aggregation of washed platelets as well as platelets in citrated and hirudin plasma. TRAP-14 (100 μM) increases the cytosolic calcium concentration in isolated guinea pig pulmonary smooth muscle cells 5-fold over baseline. It increases pulmonary arterial pressure in isolated guinea pig lung when used at a concentration of 1 μM, which is comparable to the effect induced by 10 nM α-thrombin. TRAP-14 also induces contraction of isolated rat aortic rings and increases endothelin-1 (ET-1) levels in a dose-dependent manner, an effect that is reversed by the ETA antagonist BQ-123 and the nitric oxide synthase (NOS) inhibitor L-NNA .

APJ receptor agonist 7 (compound 37) is an orally active apelin receptor (APJ) agonist with a Ki of 0.059 μM and an arrestin EC50 of 0.063 μM.

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).

NMDA receptor antagonist 4 (IIc) is an uncompetitive, voltage-dependent, orally active NMDAR blocker with an IC50 of 1.93 μM. It shows positive predicted blood-brain-barrier (BBB) permeability and can be used in Alzheimer's disease research[1].

CB1/2 agonist 4 (compound 24) is a CB1 full agonist (EC50: 15.09 nM) and a CB2 partial agonist (EC50: 1.16 nM). CB1/2 agonist 4 has significant anti-harm-sensing activity and also activates cannabinoid and TRPV1 receptors (IC50: 0.8 μM, EC50: 0.12 μM). , EC50: 0.12 μM).

mGlu4 receptor agonist 1 (compound 62) is a potent positive allosteric modulator of mGlu4 receptors, with an EC50 of 308 nM, and exhibits significant anxiolytic and antipsychotic properties [1].

TLR7 8 agonist 4 hydroxy-PEG10-acid [compound 9] is a drug-linker conjugate used in antibody-drug conjugates (ADC), exhibiting remarkable antitumor activity. It utilizes TLR7 8 agonist 4, a potent activator of TLR7 8, linked to hydroxy-PEG10-acid via a cleavable bond, demonstrating promising pharmaceutical potential in ADC-based therapeutics.

Orexin 2 Receptor Agonist 2 (ORA-2) is a specific agonist for the orexin 2 receptor.

S1P1 agonist 4 exhibits enhanced potency with an EC 50 value of less than 0.05 mg/kg and a predicted human half-life (t1/2) of approximately 5 days, indicating a favorable pharmacological profile.

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.

Glucocorticoid Receptor Agonist-4 Ala-Ala-Mal (Compound Preparation 9) is a conjugate of anti-human TNFα antibody and glucocorticoid receptor agonist (GC). It is applicable in the research of autoimmune and inflammatory diseases [1].

Protease-Activated Receptor-4 (PAR4) is a proteinase-activated receptor-4 agonist used in antiplatelet therapy.

RXFP1 receptor agonist-5 (Example 98) is an agonist targeting the RXFP1 receptor, inhibiting cAMP production in HEK293 cells with stable human RXFP1 expression, with an EC50 of 1.3 nM [1].

Compound DL5, also known as Glucocorticoid receptor modulator 4, acts as a conjugate of linkers and glucocorticoid receptor regulators. It demonstrates GRE reporter activity in K562 cells expressing mTNF with an EC50 of 40 μM. Additionally, Compound DL5 binds to anti-tumor necrosis factor (TNF) antibodies and exhibits anti-inflammatory properties in combating arthritis in mouse models.

Dopamine D3 receptor agonist 13a selectively targets the dopamine D3 receptor over dopamine D1, D2, and D4 receptors, with affinities (Ki values) of 0.14, 4,600, 2.85, and 756 nM, respectively. It also interacts with serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2A, 5-HT2B, and 5-HT2C, with Ki values of 6, 54, 1.47, and 252 nM, respectively. While acting as a partial agonist at dopamine D2 receptors (EC50 = 2.26 nM in a G protein recruitment assay), it serves as an antagonist at dopamine D3 receptors (IC50 = 4.62 nM). Additionally, Dopamine D3 receptor agonist 13a, at a dose of 3 mg/kg, has been shown to reduce cocaine self-administration in rats.

A3AR agonist 4, an A3 adenosine receptor (A3AR) agonist, exhibits an inhibitory affinity (K i) of 1.24 nM for hA3AR and dampens cAMP production with an EC 50 value of 0.17 nM. It is utilized in the study of inflammation and pain [1].

Compound 4c, also known as ABA receptor agonist 1, activates abscisic acid (ABA) receptors. It effectively inhibits seed germination and seedling growth in Arabidopsis and rice, and enhances stomatal closure and drought resistance in wheat and soybean [1].

Androgen receptor degrader-4 (compound 99) is a potent androgen receptor degrader, demonstrating an IC 50 of 3 nM. This compound effectively inhibits the proliferation of prostate cancer cells [1].

GLP-1 Receptor Agonist 11 (compound 3) acts as an effective agonist for the GLP Receptor, finding use in research related to conditions like diabetes and non-alc. fatty liver disease [1].

GPR120 Agonist 4 (example 1), a GPR120 agonist, exhibits EC50 values of 1 μM for β-arrestin A and 0.35 μM for Calcium A. This compound is utilized in research related to type II diabetes mellitus [1].

TLR7 8 agonist 4 TFA (compound 41) is a highly potent TLR7 8 agonist demonstrating significant anti-cancer activity.

PPARγ agonist 4 (Compound 18b), a potent and selective PPARγ agonist, demonstrates antitumor efficacy only when used in conjunction with Imatinib and does not exhibit cytotoxic effects on either non-resistant or resistant cells [1].

Compound 5, a selective GPR109a agonist, exhibits a pEC50 value of 5.53 [1].

STING agonist-4 is an agonist of stimulator of Interferon Genes (STING) receptor(IC50 of 20 nM).