Neurological Disease

NecroX-2 is a potent inhibitor of caspase-independent necrosis. NecroX-2 exhibits antioxidant activity by scavenging DPPH radicals and peroxynitrite. NecroX-2 inhibits t-BHP-induced mitochondrial ROS/RNS generation, and protects t-BHP and Doxorubicin (HY-15142A)-induced cell death in vitro. NecroX-2 can be used for research on neurological diseases.

LY 88329 is a potent narcotic antagonist.

JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged mGlu5 receptor negative allosteric modulator. Uncaging of JF-NP-26 is elicited with light pulses in the visible spectrum (405 nm). JF-NP-26 induces light-dependent analgesia in models of inflammatory and neuropathic pain in freely behaving animals.

KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC₅₀ of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research.

Neridronate sodium is a bisphosphonate. Bisphosphonates initiate the Apoptotic process. Neridronate sodium reduces the levels of bone resorption, bone turnover markers, the degree of back pain, and the risk of fractures. Neridronate sodium inhibits capillary tube formation. Neridronate sodium itself has weak anticancer activity, but liposomal encapsulation enhances this activity. Neridronate sodium can be used in research related to demineralizing metabolic bone diseases, thalassemia-associated osteoporosis, chronic inflammatory diseases, cancer, and osteogenesis imperfecta.

Fabomotizole dihydrochloride is an anxiolytic agent. Fabomotizole dihydrochloride produces anxiolytic and neuroprotective effects without any muscle relaxant actions.

Florbenazine (AV-133) is a diagnostic imaging agent targeting the central nervous system monoamine transporter VMAT2, and its F-18 labeled form can be used for PET scanning. The biodistribution of [18F]Florbenazine in mice shows a high striatum/cerebellum ratio (0.48), which can be used for the diagnostic research of neurodegenerative diseases (including dementia with Lewy bodies and Parkinson's disease).

HSP90-IN-18 is an effective heat shock protein 90 (Hsp90) inhibitor. HSP90-IN-18 has effective Hsp90 inhibitory activity with an IC₅₀ value of 0.39 μM. HSP90-IN-18 can be used for the research of viral infection, neurodegenerative disease, and inflammation.

6-Biopterin-d₃ (L-Biopterin-d₃) is deuterium labeled 6-Biopterin. 6-Biopterin (L-Biopterin), a pterin derivative, is a NO synthase cofactor.

Fenazinel dihydrochloride, an N-methyl-D-aspartate (NMDA) receptor antagonist, shows promise as a potential treatment for ischemic stroke.

AMG8163 is an orally active antagonist for TRPV1. AMG8163 inhibits Capsaicin (HY-10448)-induced flinch in rats models, and exhibits anti-hyperalgesia effects in multiple pain models.

(S)-Salsolidine is a weak monoamine oxidase (MAO) inhibitor (K_i=63 μM). The R enantiomer of Salsolidine is more potent than the S form (K_i=26 μM).

Atiprosine (AY-28228) is an orally effective selective α1-adrenergic receptor antagonist with a pA₂ value of 8.11. Atiprosine exhibits antagonistic activity against α2-adrenergic receptors (α1-adrenergic receptor), 5-HT₂ receptors (5-HT₂ receptor), and H₁ receptors (H₁ receptor). The pA₂ values for these receptors are 6.04, 6.87, and 7.32 respectively. Atiprosine has antihypertensive and hypotensive effects in rats, dogs, and monkeys. It can be used for research on cardiovascular and mental disorders.

Lp-PLA2-IN-5 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-5 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 32).

Itopride-d₄ (HSR803-d₄ free base) is the deuterium labeled Itopride (HY-B0732A). Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD)

MAO-A-IN-2 (Compound 4l) is a selective monoamine oxidase A (MAO-A) inhibitor with an IC₅₀ value of 0.4 μM. MAO-A-IN-2 reduces the degradation of monoamine neurotransmitters (e.g., serotonin, norepinephrine). MAO-A-IN-2 is promising for research of neurological diseases related to monoamine neurotransmitter imbalance such as depression and anxiety disorders.

FGH31 (Compound 24) is a potent, selective, GRK2 dependency dopamine D4 agonist, with the K_i of 1.6 nM. FGH31 partial activates β- arrestin.

(±)-PPCC oxalate is a sigma-1 agonist that mainly interacts with sigma-1 receptors with K_i of 1.5 nM. (±)-PPCC oxalate has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats.

PCC0105005 is a dual-target CGRP Receptor antagonist (IC₅₀ = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC₅₀ = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine.

Mirodenafil (Standard) is the analytical standard of Mirodenafil. This product is intended for research and analytical applications. Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).