st 4

Adenosine receptor antagonist 4 is an adenosine receptor antagonist.

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 Conjugate is a conjugate of MC-Val-Cit-PAB-Amide and TLR7 agonist 4, used in cancer research.

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 TFA is the trifluoroacetate form of MC-Val-Cit-PAB-Amide-TLR7 agonist 4. MC-Val-Cit-PAB-Amide-TLR7 agonist 4 is a HER2-TLR7 and HER2- TLR8 immune agonist complexes with potential antitumor activity by activating the TLR7 and TLR8 signaling pathways and enhancing immune responses.

AHR antagonist 4 is a potent aryl hydrocarbon receptor (AHR) antagonist(example 293; IC50: 82.2 nM).It has anti-cancer effects.

AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.

CB1 antagonist 4 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.

Calcium Channel antagonist 4 is a voltage-gated calcium channel inhibitor (IC50 : 5-20 μM).

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.

CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist with IC50 values of 180 nM and 24 nM for CCR2 inhibition and MCP-1-induced chemotaxis inhibition, respectively.

FPR Agonist 43 is a dual agonist of formyl peptide receptor 1 and formyl peptide receptor 2 (FPR2) ALX.

CCR2 antagonist 4 hydrochloride is a specific CCR2 antagonist (IC50s: 180 nM for CCR2b). It potently inhibits MCP-1-induced chemotaxis (IC50: 24 nM).

H3R antagonist 4 (compound 11l) serves as a dual inhibitor of cholinesterases and histamine H3 receptors (H3R), demonstrating IC50 values of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible), and 1.09 nM (H3R). It effectively inhibits both self and Cu2+-induced Aβ1-42 aggregation at 95.48% and 88.63%, respectively, and degrades Aβ1-42 protofibrils with 80.16% and 89.30% efficiency under similar conditions. Additionally, H3R antagonist 4 possesses the chelating capability for biometals Cu2+, Zn2+, Al3+, and Fe2+. It significantly reduces tau protein hyperphosphorylation induced by Aβ1-42, inhibits RSL-3 induced apoptosis and ferroptosis in PC12 cells, and shows optimal blood-brain barrier permeability and intestinal absorption characteristics in hCMEC D3 and hPepT1-MDCK cells, respectively. Moreover, the compound improves learning and memory impairments in an Alzheimer's mouse model induced with scopolamine.

KOR agonist 4 (compound 39) is an agonist targeting the κ opioid receptor (Kappa Opioid Receptor) and activates G protein signaling. It has an EC50 of 14 nM and an Emax of 83% for binding to GTPγS. This compound demonstrates moderate to high intrinsic clearance in human liver cells and shows selectivity for the κ opioid receptor over the μ (MOR) and δ (DOR) opioid receptors by factors of 60 and 810, respectively. KOR agonist 4 is useful for research into central nervous system (CNS) disorders.

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.

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.

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

TLR7 8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate used in antibody-drug conjugates (ADCs) with high tumor efficacy. It consists of TLR7 8 agonist 4, a potent TLR7 8 agonist, linked to the ADC linker hydroxy-PEG10-acid, which can be cleaved.

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].

Wnt β-catenin agonist 4 is an agonist of Wnt that activates Wnt β-catenin signaling and directs signaling.

EP4 receptor antagonist 4 is an agonist of EP4 receptor (human pEC 50 = 6.3) [1].

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

SSTR4 agonist 4 is a potent SSTR4 agonist with potential applications in pain research. SSTR4 agonists demonstrate efficacy in rodent models of pain associated with acute and chronic anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, regions involved in memory and learning, and in Alzheimer's disease pathology [1].

Androgen receptor antagonist 4 (Compound AT2) exhibits anticancer activities by potently antagonizing AR transcriptional activity, inhibiting downstream AR target genes, and blocking DHT-induced nuclear translocation of AR. It is an antagonist of the androgen receptor (AR) with an IC50 of 0.15 μM [1].

CXCR2 antagonist 4 (compound 7) is a highly potent inhibitor of CXCR2 with an IC50 of 0.13 μM and effectively inhibits the CXCL8-induced cytosolic calcium increase with an IC50 of 27 μM, demonstrating promising potential for anticancer research [1].