glucocorticoid receptor agonist

Glucocorticoid receptor agonist is an effective glucocorticoid receptor agonist.

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

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].

Glucocorticoid Receptor Agonist-4 (Compound Preparation 5) serves as an agonist for glucocorticoid receptors and can be conjugated with TNF-α antibodies, facilitating research into autoimmune and inflammatory diseases [1].

Glucocorticoid Receptor Agonist-3 (Preparation 6) acts as a glucocorticoid receptor agonist [1].

Glucocorticoid Receptor Agonist-1 Phosphate (Gly-Glu-Br) is an antibody-drug conjugate (ADC) linker utilized in the synthesis of ABBV-154, ABBV-927, ABBV-368, and related analogs [1].

Glucocorticoid Receptor Agonist-1 Phosphate Ala-Ala-Mal functions as a glucocorticoid receptor agonist, utilized in the formulation of anti-CD40 antibody agent conjugates (ADC). It serves as a research tool for exploring inflammation and immune regulation [1].

Glucocorticoid receptor agonist-2 Ala-Ala-Mal (compound 79) serves as a precursor for synthesizing anti-inflammatory antibody-drug conjugate (ADC) molecules and acts as an active reference for ABBV-3373 [1].

Compound 9E, a Glucocorticoid receptor agonist-1-Gly-Glu-Gly, serves as a steroid-linker conjugate designed for the synthesis of Antibody-Drug Conjugates (ADCs) [1].

Glucocorticoid Receptor Agonist-1 Phosphate Gly-Glu (TFA) serves as a cleavable linker for the synthesis of Antibody-Drug Conjugates (ADCs).

Glucocorticoid Receptor Agonist-1 Phosphate Ala-Ala-Br is a drug-linker conjugate for antibody-drug conjugates (ADCs), serving as a reaction reagent in the creation of anti-CD40 antibody agent conjugates [1].

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].

Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Mal functions as a glucocorticoid receptor agonist and serves as a drug-linker conjugate for ADC. This compound is instrumental in the synthesis of anti-CD40 antibody agent conjugates (WO2019106608A1; example 9) [1].

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-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.

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.

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

Glucocorticoids receptor agonist 1 (GRA-1) is a highly effective arylpyrazole-based compound that acts as an agonist for the glucocorticoid receptor. GRA-1 exhibits strong anti-inflammatory properties while maintaining insulin secretion function.

Glucocorticoid receptor agonist 2 is a highly effective anti-inflammatory compound, derived from arylpyrazole, that actively binds to and activates the glucocorticoid receptor. This compound exhibits potent anti-inflammatory properties without disrupting insulin secretion.

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].

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].

Glucocorticoid receptor modulator 1 is a potent, orally active, non-steroidal selective glucocorticoid receptor modulator, exhibiting IC50 values of 9 nM and 130 nM against NF-κB and AP-1, respectively. It effectively reduces the expression of inflammatory factors such as IL-6, IL-1β, and TNF-α, and alleviates dermatitis in mice.

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).

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].

Glucocorticoid receptor-IN-1 is a selective regulator of the glucocorticoid receptor (GR) and exhibits anti-inflammatory activity. glucocorticoid receptor-IN-1 has good transcriptional repression, acting on hMMP1 ( IC50: 2.11 nM) and also has a transcriptional activating effect on MMTV (EC50: 5.59 nM).

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

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.

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.

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].

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].

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

Compound (S)-9, a GLP-1 receptor agonist, exhibits an EC50 of 76 nM for the glucagon GLP-1 receptor [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].

EP4 receptor agonist 2 (compound 31) is a potent EP4 receptor agonist, demonstrating an EC50 value of 0.8 nM and K_i values of >100,000, 38,000, and 3.1 nM for the EP2, EP3, and EP4 receptors, respectively [1].