Neurological Disease

Zicronapine (Lu 31-130) fumarate is an antipsychotic agent with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine (Lu 31-130) fumarate has potent antagonistic effects at dopamine D1/D2, and serotonin 5-HT2A receptors.

HCN2-IN-2 (Compound 35), azaindazole derivative, is a selective HCN2 inhibitor with an IC₅₀ of 145 nM. HCN2-IN-2 inhibits HCN2 channel activity blocks abnormal firing of peripheral nociceptive neurons. HCN2-IN-2 can be used for the research of pain.

Protriptyline-d₃ is deuterium labeled Protriptyline (HY-B0949). Protriptyline is a potent tricyclic antidepressant (TCA). Protriptyline inhibits AChE activity with an IC₅₀ value of 0.06 mM and inhibits Aβ self-assembly. Protriptyline can be used for the study of depression and Alzheimers disease.

Varenicline-d₄ is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment.

TGN, Cys modified is a cysteine modified TGN (HY-P11284) on the C-terminus. TGN, a 12-amino acid ligand, is a BBB-penetrating peptide. TGN can be used as a drug delivery vehicle for Alzheimer's disease research.

Erianin (Standard) is the analytical standard of Erianin. This product is intended for research and analytical applications. Erianin, often used as an antipyretic and analgesic agent, could inhibit IDO-induced tumor angiogenesis.

Illudinine, a sesquiterpenoid alkaloid, is a monoamine oxidase B (MAO-B) inhibitor with an IC₅₀ of 18.3 μM. Illudinine can be used for research on neurological diseases.

C26-Dihydro ceramide is a dihydroceramide containing a C26 very-long-chain fatty acid. C26-Dihydro ceramide can be used for research on various neurological disorders including Alzheimer's disease, Parkinson's disease, multiple sclerosis, depression, and anxiety disorders.

Tracizoline is an orally active I2-imidazoline receptor agonist. Tracizoline functionally modulates I2-imidazoline receptors, regulates hippocampal FADD cell fate adaptor, attenuates mechanical and thermal hyperalgesia, activates α₂A-adrenergic receptors with very weak partial agonism, and induces antidepressant-like activity via 5-HT₁A receptor activation. Tracizoline can be used for the research of inflammatory pain, neuropathic pain, and depression.

Paroxetine-d₂ (BRL29060-d₂) is the deuterated-labeled Paroxetine (HY-122272). Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

YM-796 dihydroxybutanedioate is a selective muscarinic M₁ receptor agonist. YM-796 dihydroxybutanedioate can improve cognitive impairment and reduce amyloid plaque deposition. YM-796 dihydroxybutanedioate can be used in the research of cognitive impairment diseases such as Alzheimer's disease.

Azocarnil is a GABAergic agonist-potentiator. Azocarnil can be used in neurological research.

PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with K_is of 2 and 5 nM against PARP-2 and PARP-1, respectively. PARP-2/1-IN-2 has an EC₅₀ of 3 nM in a cell based assay of PARP activity.

JNJ-54082730 (Compound 1) is the orally active inhibitor for phosphodiesterase (PDE) that inhibits PDE2A, PDE3B, and PDE10A2 with IC₅₀s of 0.95 nM, 6.17 μM (pIC₅₀=5.21) and 87.1 nM (pIC₅₀=7.06), respectively. JNJ-54082730 modulates the activity of AMPA receptor, enhance the synaptic plasticity and promotes the learning and memory function in rats models. JNJ-54082730 can cross blood-brain barrier.

SLV-317 is an antagonist of the neurokinin-1 receptor with oral activity. SLV-317 can effective antagonist of substance P-induced effects.

Q14 is a polypeptide derived from the USP30 (ubiquitin specific peptidase 30) transmembrane (TM) domain with the ability to inhibit the deubiquitination activity of USP30 (IC₅₀=57.2 nM). Q14 reduces USP30 activity by inhibiting the interaction between the USP30 transmembrane domain and its catalytic domain. Q14 peptide contains the LC3 interaction region (LIR) motif, which enables it to bind to the LC3 and accelerate the formation of autophagosomes, thereby promoting mitophagy. Q14 can be used in the study of neurodegenerative diseases as well as mitochondrial quality control and cell metabolism.

NK3R antagonist-2 (Compound 45) is a small-molecule antagonist of tachykinin NK3R, with an IC₅₀ of 1100 nM and a K_i of 1800 nM. NK3R antagonist-2 can be used in the research of schizophrenia.

Fonagepant (FE 205030) is a calcitonin gene-related peptide (CGRP) receptor antagonist with an IC₅₀ of 0.2 nM. Fonagepant selectively blocks CGRP receptor activity, inhibits CGRP-induced vasodilation, attenuates capsaicin-induced increase in skin blood flow, and blocks CGRP-induced vasodilation in isolated human mesenteric resistance arteries. Fonagepant can be used in studies related to acute migraine attacks.

Protopine (Standard) is the analytical standard of Protopine. This product is intended for research and analytical applications. Protopine (Corydinine), an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity.

HTL-9936 is an orally active partial agonist of muscarinic M1 receptor. HTL-9936 has an EC₅₀ of 32 nM for human M1 receptor and an EC₅₀ of 224 nM for human M4 receptor. HTL-9936 activates Gq/11 coupling, promotes inositol phosphate accumulation, ERK1/2 phosphorylation, β-arrestin recruitment and receptor internalization. HTL-9936 can be used in the research of Alzheimer's disease and schizophrenia.