Neurological Disease

Tyr0-Neurokinin B (Tyr-NKB) is an analogue of Neurokinin B. Tyr0-Neurokinin B can exerts contractions in bladder.

FK 453 (compound 1d) is a potent and selective adenosine A1 receptor antagonist with an IC₅₀ value of 17.2 nM.

β-Pompilidotoxin TFA (β-PMTX TFA), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.

JGK-263 is an orally active Glycogen synthase kinase-3β (GSK-3β) inhibitor. JGK-263 exhibits neuroprotective effect and can improve motor function. JGK-263 can be used for the research of neurological disease, such as amyotrophic lateral sclerosis (ALS).

α-Synuclein inhibitor 5 (compound 4aa) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC₅₀ of 1.22 μM and inhibition ratio at 30 μM of 94.3%.

P-Hydroxybenzaldehyde-¹³C₆ is the ¹³C-labeled p-Hydroxybenzaldehyde (HY-Y0313). p-Hydroxybenzaldehyde is a one of the major components in vanilla aroma, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.

CCK2R agonist-1 (Compound 2S) is a CCK2R agonist, with an IC₅₀ of 48 nM against wild-type CCK-2R and an IC₅₀ of 450 nM against mutant CCK-2R (N353L). CCK2R agonist-1 stimulates the production of inositol phosphate. The changes in pH and HDC induced by CCK2R agonist-1 in mice are comparable to those induced by the full-length peptide agonist Gastrin. CCK2R agonist-1 can be used in studies of gastric diseases and pain.

3,4-Methylenedioxy PV8 hydrochloride is a pyrrolidine-containing synthetic drug derivative.

JNJ-42259152 is a phosphodiesterase 10A (PDE10A) positron emission tomography (PET) tracer that is specific for PDE10A activity. JNJ-42259152 can be dynamically scanned in healthy volunteers to assess its kinetic properties in the brain. The half-life of JNJ-42259152 in the blood is an average of 90 minutes. JNJ-42259152 has demonstrated reliable binding potential (BPND) in different target areas (such as the lentiform nucleus, caudate nucleus, ventral striatum, etc.), providing an important tool for studying neuropsychiatric diseases.

Cyclo(Gly-Pro) is a cyclic dipeptide. Cyclo(Gly-Pro) can be derived from the Nterminus of the IGF-1. Cyclo(Gly-Pro) attenuates nociceptive behaviour and inflammatory response in mice.

Meclofenamic acid (Meclofenamate) sodium hydrate is a non-steroidal anti-inflammatory agent. Meclofenamic acid sodium hydrate is a highly selective FTO (fat mass and obesity-associated) enzyme inhibitor. Meclofenamic acid sodium hydrate competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid sodium hydrate is a non-selective gap-junction blocker. Meclofenamic acid sodium hydrate inhibits hKv2.1 and hKv1.1, with IC₅₀ values of 56.0 and 155.9 μM, respectively.

BuChE-IN-4 (Compound C6) is a potent inhibitor of BuChE with an IC₅₀ of 7.7 nM. BuChE-IN-4 exhibits mild antioxidant capacity, nontoxicity, lipophilicity and neuroprotective activity.

PROTAC LRRK2 Degrader-2 is a PROTAC-based degrader targeting LRRK2 with a DC₅₀ of 0.14 nM. PROTAC LRRK2 Degrader-2 recruits LRRK2 or its mutants to the cereblon E3 ubiquitin ligase, thereby mediating the targeted ubiquitination and subsequent proteasomal degradation of LRRK2. PROTAC LRRK2 Degrader-2 can be used in research related to Parkinson's disease.

5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT₆/5-HT_2A receptor antagonist, with a K_i of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties.

U-89843A (PNU-89843) is a GABAA receptors positive allosteric modulator (PAM). U-89843A enhances GABA-induced Cl^- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. U-89843A shows antioxidant and sedative effects.

HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC₅₀ values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease.

VU0606170 is a selective Slack channel inhibitor with low micromolar potency. VU0606170 can reduce the frequency of neuronal Calcium oscillations in a concentration dependent manner. VU0606170 can be used for research on diseases such as epilepsy.

TRKB(NTRK2) is a member of tyrosine kinase gene family. TRKB is the primary receptor for brain-derived nerve growth factor (BDNF) and neurotrophin 4/5 (NT4/5). TRKB(NTRK2) Recombinant Human Active Protein Kinase is a recombinant TRKB(NTRK2) protein that can be used to study TRKB(NTRK2)-related functions.

COX-2/HDAC6-IN-1 (Compound 11e) is a dual COX-2 and HDAC6 inhibitor, with an IC₅₀ of 0.12 μM against HDAC6 and an IC₅₀ of 0.66 μM against COX-2. COX-2/HDAC6-IN-1 enhances the acetylation level of α-tubulin, regulates epigenetic gene expression, and inhibits the expression of pro-inflammatory mediators (COX-2, IL-1β, IL-6 and TNF-α). COX-2/HDAC6-IN-1 promotes Amyloid-β clearance and reduces excessive phosphorylation of Tau protein. COX-2/HDAC6-IN-1 maintains neuronal morphology by stabilizing MAP2, protects synaptic integrity by regulating synapsin, and restores the expression of memory-related genes. COX-2/HDAC6-IN-1 possesses neuroprotective activity and improves learning and memory abilities in Scopolamine (HY-N0296)-induced Alzheimer's disease mouse models. COX-2/HDAC6-IN-1 is applicable to research related to Alzheimer's disease.

BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC₅₀s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu²⁺, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s disease.