adenosine a1 receptor activator t62

Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor, and it produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409/22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409/22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

CCR1/5/8 activator 1 is a cytoplasmic phospholipase A inhibitor with antifungal activity.

Adenosine antagonist-1 acts as an adenosine A3 receptor (AA3R) antagonist.

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

(2E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,6,10,14-tetraen-1-yl dihydrogen diphosphate,tetrabutylammonium(1:1.5) is a common precursor of taxadiene such as Paclitaxel.

Adenosine receptor A1 antagonist 5 acts as an adenosine antagonist, is an oxypurine, acts as an insecticide and pest control agent, and has an inhibitory effect on elevated blood pressure.

1-ethyl-6-fluoro-4-oxo-7-[4-(3-phenylpropanoyl)piperazin-1-yl]-1,4-dihydroquinoline-3-carboxylic acid is a compound used as a molecular structural unit and is a SMURF1 inhibitor.

Thrombin Receptor Activator for Peptide is also called Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), used in the research of coronary heart disease (CHD).

Geranylgeranyl pyrophosphate tetrabutylammonium(1：2) is one of the endogenous cholesterol and intermediates produced by the mevalerate pathway. Geranylgeranyl pyrophosphate tetrabutylammonium(1：2) is the common precursor of diterpenoids, for example, Paclitaxel. It can be used for cancer research.

A2B receptor antagonist 1 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.

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].

AMPA receptor modulator-1 can be activated by glutamate, thereby modulating ion channels.

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

Potassium Channel Activator 1 can be used in studies about the treatment of disorders or conditions wherein the dopaminergic system is disrupted such as mood disorders ADHD, schizophrenia, and other psychotic states.

LPA1 receptor antagonist 1(LPA1 R antagonist 1) is a selective and potent lysophosphatidic acid (LPA1) receptor antagonist (IC50 : 25 nM) for the study of idiopathic pulmonary fibrosis.

NAMPT Activator-1 (compound 1) is an effective and specific activator of niacinamide phosphotransferase (Compound 1) with a wide range of EC50 (3.3-3.7 μM). NAMPT activator-1 effectively protects cultured cells from FK866-mediated toxicity and is a potential neuroprotective compound.

A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.

Dopamine D2 Receptor Antagonist-1 functions as a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), demonstrating sub-millimolar affinity.

Sigma-1 receptor antagonist 2 is a potent and selective antagonist of sigma 1 receptor (σ1 R) (σ1 and σ2 receptor with Kis of 3.88 and 1288 nM , respectively).

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

Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM. GABAB receptor antagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

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

GABA receptor Antagonist 1 (compound 7w) effectively inhibits the Px RDL1 GABAR at an IC50 of 7.08 nmol/L and demonstrates insecticidal efficacy against P. xylostella, S. frugiperda, S. exigua, and S. litura with respective LC50 values of 0.09, 0.84, 0.87, and 0.68 mg/L. Moreover, this compound exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg/adult) and low toxicity to zebrafish (LC50: 42.4 mg/L) [1].

Interferon receptor inducer-1 Used in the treatment of a disorder in which the induction of interferon is involved. is an interferon (IFN) receptor inducer.

Caspase-3 activator 1 (compound 4b), a Ru(III) metal complex, effectively inhibits gastric tumor growth and metastasis by mediating caspase-3 cleavage. This cleavage enables Caspase-3 to process gasdermin E (GSDME), which results in the production of the GSDME-N terminus, leading to perforation of the gastric tumor cell membrane. Furthermore, compound 4b induces pyroptosis and subsequent immune responses. It can be incorporated with decitabine (DCT) into the 4b-DCT-Lip lipid delivery system [1].

Androgen Receptor Degrader-1 (Compound 18) is a potent agent for androgen receptor degradation, applicable in cancer research [1].

RXFP1 receptor agonist-1 (Example 2), an agonist of the RXFP1 receptor, suppresses cAMP production in HEK293 cells that constitutively express the human RXFP1, exhibiting an EC50 of 300 nM [1].

AMPK-α1β1γ1 activator 1 (M1), an acyl glucuronide metabolite derived from an Indole-3-carboxylic Acid-based AMPK activator, selectively activates the β1 isoforms of human AMPK with an EC50 of 38.1 nM through direct binding to the human AMPK α1β1γ1 isoform. It is utilized in diabetic nephropathy research [1].

Thrombin Receptor Activator for Peptide 5 (TRAP-5), also known as Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), is employed in coronary heart disease (CHD) research.

Histamine H4 receptor antagonist-1 is a potent antagonist of the histamine H4 receptor.

GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist , has an EC50 of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes.

Succinate/succinate receptor antagonist 1 is a potent succinate receptor antagonist. Succinate/succinate receptor antagonist 1 interrupts succinate signals in gingival tissue and inhibits the activation of SucnRl Antagonist 1. Its IC50 value is 20 μsouth of the coast. Succinate/succinate receptor antagonist 1 can be used to treat periodontal disease.

SIRT1 Activator 1 (Compound 3), a marine-derived xyloallenoide A derivative from the Xylaria sp. mangrove fungus, exhibits angiogenic effects in zebrafish and protects human endothelial progenitor cells (hEPCs) from AngII-induced senescence. It achieves this by elevating SIRT1 expression and modulating the AMPK/Akt signaling pathway [1].

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

T-1-MCPAB, a VEGFR-2 inhibitor with an IC50 of 0.135 µM, effectively suppresses MCF7 cell migration and has applications in cancer research [1].

β2AR/M-receptor agonist-1 (example 131), a muscarinic antagonist and β2 adrenoceptor agonist (MABA), exhibits dual potency towards β2 adrenoceptor and muscarinic receptor. It demonstrates a significant affinity for the β2 adrenoceptor, indicated by an EC50 value of 9.2 nM, and for the muscarinic receptor with a Ki value of 30.2 nM. Furthermore, its MABA activity is highlighted by an EC50 value of 4.0 nM [1].

Adenosine receptor antagonist 4 is an adenosine receptor antagonist.

Nrf2 activator-1 is a potent activator of NF-E2-related factor 2 (Nrf2).Nrf2 activator-1 can be used to study COPD and other respiratory diseases including asthma, acute lung injury (ALI), acute respiratory distress syndrome (ARDS), and pulmonary fibrosis.

σ1 Receptor antagonist-1 is a selective sigma 1 receptor antagonist.

αvβ1 integrin-IN-1 TFA is an effective and selective αvβ1 integrin inhibitor (IC50: 0.63 nM).

1-(t-Boc-Aminooxy)-3-aminooxy-propane is an alkyl/ether-based PROTAC linker utilized in the synthesis of PROTACs[1].

3'-O-t-Butyldimethylsilyl adenosine is a Nucleoside; Used for special nucleoside modification.

Vanilloid receptor antagonist 1 (4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile) is a potent vanilloid receptor TRPV1 antagonist.

A1/A3 AR antagonist 1 (Compound 10) is a potent, dual adenosine 1 (A1) and adenosine 3 (A3) receptor antagonist that acts on human A1 (Ki: 37.6 nM), human A3 (Ki: 25.4 nM) and rat A1 (Ki: 1.47 nM). 1 Can be used to study renal failure, inflammatory lung disease and Alzheimer's disease.

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.

A2A/A1 AR antagonist-1 (compound 1a) has the potential for ischemic stroke research which is potent A 2A /A 1 AR dual antagonist with Ki s of 5.58 and 24.2 nM, respectively [1].