orexin 2 receptor agonist

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

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

TREM2 agonist-2 (I-192) is an orally active and potent agonist of myeloid triggered receptor 2 (TREM2) for neurodegenerative disease research.

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.

Edg-2 receptor inhibitor 1 (SAR-100842) is an Edg-2 receptor inhibitor extracted (IC50: <0.1 μM).

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.

A2B receptor antagonist 2 hydrochloride is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

AMPA receptor antagonist-2 is an AMPA receptor antagonist.

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.

S1R agonist 2 is a selective S1R agonist with a Ki of 88 nM for S2R and 1.1 nM for S1R and is protective against ROS and NMDA-induced neurotoxicity.

AMPA receptor modulator-2 (Example 134) is an AMPA receptor modulator with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor[1]. pIC50 = -lgIC50. [1]. BERRY CYNTHIA G B (US), et al. AZABENZIMIDAZOLES AND THEIR USE AS AMPA RECEPTOR MODULATORS. Patent. WO2016176460.

HIF-2α agonist 2 is an HIF-2α agonist with an EC50 value of 1.68 μM for HIF-2α. HIF-2α agonist 2 can promote the stability of the ARNT A B ring in the 3z structure of HIF-2a-ARNT complex without cytotoxicity to 786-o-Reha-Luc cells. HIF-2α agonist 2 can be used in the study of oxygen metabolism and is closely related to the occurrence of cancer.

GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively.

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

Sigma-1 receptor antagonist 2 is a more potent and selective antagonist of the sigma-1 receptor (σ1 R, Ki = 3.88 nM) compared to the sigma-2 receptor (Ki = 1288 nM).

TLR7 agonist 2 (TLR7-IN-1) is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).

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

GPR120 Agonist 2 is a potent and selective GPR120 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.

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

GPCR agonist-2 (4-(Cyclopropylamino)-3-nitrobenzoic acid) is an agonist of the orphan human GPCR GPR109B.

Protease-Activated Receptor-2, amide (SLIGKV-NH2) is an agonist of PAR2 with an IC50 of 10.4 M.

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].

Compound 17, a dopamine D4 receptor ligand, exhibits high potency and selectivity with IC 50 values of 0.057 nM for D4, and >1000, 220, and 270 nM for D2, 5-HT1A, and α1 receptors, respectively [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].

ET Receptor Antagonist 2 (Compound 16j) is an orally active ET receptor antagonist with an IC50 of 0.22 nM, suitable for pulmonary arterial hypertension (PAH) research. It has been shown to mitigate monocrotaline-induced PAH in a rat model [1].

Compound 28.1, also known as TAS2R14 agonist-2, is a potent and selective inhibitor of TAS2R14, exhibiting an EC50 of 72 nM [1].

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].

Cisd2 agonist 2 (compound 6), with an EC50 of 191 nM, is an orally active activator of Cisd2, a protein whose levels are associated with nonalcoholic fatty liver disease (NAFLD). In vivo studies have demonstrated that Cisd2 agonist 2 exhibits no significant toxicity in heterozygous hepatocyte-specific Cisd2 knockout (Cisd2hKO-het) mice [1].

GPR139 agonist-2 (compound 20a), a potent GPR139 agonist with an EC50 of 24.7 nM, has demonstrated efficacy in rescuing social interaction deficits and alleviating cognitive deficits in murine schizophrenia models, indicating its potential in antischizophrenia drug research [1].

GPR40 Agonist 2 is a compound that functions as a GPR40 agonist and is utilized in diabetes research.

GPR81 agonist 2 is a potent agonist targeting the GPR81 receptor, demonstrating EC50 values of 0.023 µM for hGPR81 and 0.123 µM for hGPR109A, respectively.

Protease-Activated Receptor-1 Antagonist 2 is an orally active antagonist of protease-activated receptor-1 (PAR-1), demonstrating significant potency with an IC 50 of 7 nM. It exhibits favorable pharmacokinetic characteristics, making it valuable in cardiovascular disease (CVD) research, including studies on atherosclerosis and restenosis [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].

EGF Receptor Substrate 2 (Phospho-Tyr5) is a biologically active peptide derived from an autophosphorylation site (Tyr 992 ) of epidermal growth factor receptor (EGFR).

ERRγ agonist-2 is a potent and selective ERRγ inverse agonist with a Kd value of 6.5 μM, inhibiting the expression of hepcidin, fibrinogen, and gluconeogenic genes. ERRγ agonist-2 exhibits antimicrobial, anti-coagulant, and antidiabetic activities [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.

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).

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].

FPR2 agonist 2 is a potent FPR2 agonist with blood-brain barrier permeability that acts on h-FPR2 (EC50: 0.13 nM), inhibiting the production of pro-inflammatory cytokines, counteracting changes in mitochondrial function, and inhibiting caspase-3 activity.

NMDA receptor antagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound is valuable in scientific investigations of neuropathic pain and Parkinson’s disease.

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.