Neurological Disease

N-Desmethyl-U-47700 is the primary metabolite of U-47700 (an opioid agonist).

SGE-201 is an allosteric modulator of N-methyl-D-aspartate receptors (NMDARs), demonstrating significant neuroprotective effects by enhancing NMDAR-mediated responses while differing in action among various blockers in neuronal networks.

Glutaminyl Cyclase Inhibitor 2 is a glutaminyl cyclase inhibitor with an IC₅₀ of 1.23 μM.

Stigmane B (Compound 2) is a nuclear factor E2-related factor (Nrf2) activator. Stigmane B downregulates apoptosis and reactive oxygen species (ROS) generation, and increases antioxidant enzyme activities. Stigmane B shows neuroprotective effects.

Tau-aggregation-IN-3 (compound 9) a Tau protein aggregation inhibitor (TAI). Tau-aggregation-IN-3 shows activity in cell-based aggregation inhibition experiments (EC₅₀=4.816 μM). Tau-aggregation-IN-3 can be used in Alzheimer's disease research.

2,3-Diphosphoglyceric acid-d3 ammonium (2,3-DPG-d3 ammonium) is the deuterium labeled 2,3-Diphosphoglyceric acid (HY-113050). 2,3-Diphosphoglyceric acid (2,3-DPG) is an intermediate of the glycolytic pathway. 2,3-Diphosphoglyceric acid stabilizes the deoxygenated form of hemoglobin by allosteric binding and facilitates oxygen release at tissue sites. 2, 3-diphosphoglyceric acid has antiparasitic activity. 2,3-Diphosphoglyceric acid can be used in the study of Alzheimer's disease (AD).

MSK-9 is a positive allosteric modulator of the P2X4 receptor with dual activities of enhancing ion conductance and delaying receptor inactivation. MSK-9 stabilizes the open state of the P2X4 receptor through rigid 3-piperidinyl and hydrophobic menthyl substituents. MSK-9 can be used in the study of multiple sclerosis (MS).

UK-240455 is a potent and selective N-methyl D-aspartate (NMDA) glycine site antagonist.

AC-178335 is a SRIF antagonist, with a K_i of 172 nM. AC-178335 blocks SRIF inhibition of adenylate cyclase in vitro (IC₅₀=5.1 μM). AC-178335 induces GH release in anesthetized rats.

Ibodutant (MEN 15596) is a potent and selective tachykinin NK2 receptor antagonist with a pK_i of 10.1.

Clobenpropit is a potent histamine H3-receptor antagonist. Clobenpropit decreases dopamine release and increases histamine levels in the hypothalamus. Clobenpropit shows antipsychotic-like activities. Clobenpropit causes a resuscitating effect in rats subjected to the hemorrhagic shock.

Calebin A is a PI3K/Akt/mTOR, MAPK, and NF-κB inhibitor with oral effectiveness. Calebin A can block the autophagy-repressive, inhibiting apoptosis. Calebin A has anti-tumor activity by epigenetic regulation. Calebin A suppresses adipogenesis, modulates thermogenesis, and enriches gut probiotics. Calebin A can be used in research on osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer.

AChE-IN-20 (compound M26) is a potent AChE inhibitor with IC₅₀ value of 397.32 nM and with K_i value of 335.76 nM. AChE-IN-20 shows inhibition potency against hCA I , hCA II and α-GLY with IC₅₀ values of 84.14, 69.24 and 52.08 nM and with K_i values of 97.86, 76.23 and 57.93 nM, respectively.

AM1172 is metabolically stable anandamide uptake inhibitor. AM1172 inhibits [³H] anandamide transport in rat cortical neurons and human CCF-STTG1 astrocytoma cells with IC₅₀ values of 2.1 μM and 2.5 μM, respectively. AM1172 can significantly inhibit AEA hydrolysis and concurrently decrease AEA uptake. AM1172 can be used for the study of endocannabinoid system regulation.

4-Hydroxy MPT (4-OH-MPT), a serotonergic hallucinogen, is a 5-HT2A and 5-HT2B receptors agonist with EC₅₀ values of 3.82 nM and 3.4 nM, respectively.

AChE/BChE/MAO-B-IN-4, an indan-1-one derivative, is a potent MAO-B inhibitor with an IC₅₀ of 0.0393 μM for human MAO-B. AChE/BChE/MAO-B-IN-4 is a potent AChE and BChE enzyme inhibitor, with IC₅₀s of 0.0458 μM and 0.075 μM for human AChE and BChE enzyme, respectively. AChE/BChE/MAO-B-IN-4 shows significant antioxidant activity and prevent β-amyloid plaque aggregation. AChE/BChE/MAO-B-IN-4 has the potential for Alzheimer's disease (AD) research.

Calmodulin Dependent Protein Kinase Substrate Analog is a Ca²⁺- and calmodulin (CaM)-dependent protein kinase (CaMK) substrate peptide. Calmodulin Dependent Protein Kinase Substrate Analog is a synthetic peptide substrate for protein kinases.

Nurr1 agonist 11 (compound 53) is a selective and potent Nurr1 agonist with an IC₅₀ of 26 µM. Nurr1 agonist 11 has the ability to cross a cellular model of the blood-brain-barrier (BBB) .

Nociceptin (1-13)，amide is a potent ORL1 receptor (opioid receptor-like 1 receptor，OP4) agonist with a pEC₅₀ of 7.9 for mouse vas deferens and a K_i of 0.75 nM for binding to rat forebrain membranes.

(Rac)-Vazegepant-¹³C,d₃ ((Rac)-Zavegepant-¹³C,d₃; (Rac)-BHV-3500-¹³C,d₃) is the deuterated, ¹³C-labeled Vazegepant (HY-134992). Vazegepant (Zavegepant; BHV-3500) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with a K_i of 23 pM for human CGRP receptor and an EC₅₀ of 880 pM for reversing CGRP-induced vasodilation in human intracranial arteries. Vazegepant can block CGRP-mediated vasodilation in the trigeminal vascular system and inhibit neuronal circuit sensitization. Vazegepant can be used in migraine-related research.