Neurological Disease

hCA I-IN-4 (Compound 14) is the inhibitor for carbonic anhydrase and cholinesterase, that inhibits hCA I, hCA II, AChE, and BChE with K_i of 29.94 nM, 17.72 nM, 21.21 nM, and 7.65 nMrespectively. hCA I-IN-4 exhibits cytotoxicity in BT-549 with IC₅₀ of 16.59 μM.

CLIK-148 is a highly selective, irreversible and orally active cysteine protease inhibitor, primarily targeting Cathepsin L. CLIK-148 effectively inhibits the Cathepsin L-dependent degradation of HMG-CoA reductase in the endoplasmic reticulum (ER) membrane. CLIK-148 inhibits the processing of proCCK by Cathepsin L, thereby reducing the production of CCK8 (HY-P0093). CLIK-148 inhibits the degradation of type I collagen by osteoclasts' secreted Cathepsin L, reducing tumor-induced bone metastasis and malignant hypercalcemia. CLIK-148 can be used for the studies of bone metabolism disorders and regulation of neuropeptide processing.

Azure B (Standard) is the analytical standard of Azure B. This product is intended for research and analytical applications. Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects.

GPER/Bcl-2-IN-1 is a GPER/Bcl-2 inhibitor. GPER/Bcl-2-IN-1 can inhibit the proliferation and neurospheres formation of glioblastoma cells. GPER/Bcl-2-IN-1 can be used for the study of glioblastoma multiforme (GBM).

TWIK-1/TREK-1-IN-3 (compound 2h) is an inhibitor of TWIK-related potassium channel (Potassium Channel) TREK-1. TREK-1 contains a two-pore domain potassium (K2p) channel that dimerizes into TREK-1 homodimer and TWIK-1/TREK-1 heterodimer, and is an important antidepressant target. TWIK-1/TREK-1-IN-3 targets TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC₅₀s of 9.74 μM and 16.5 μM, respectively, and has antidepressant-like effects.

α-Synuclein aggregate binder 2 (Compound 1) is a specific alpha-synuclein binder with a K_i of 1.6 nM. α-Synuclein aggregate binder 2 has a weak binding affinity for β-amyloid aggregates with a K_i of 295 nM. α-Synuclein aggregate binder 2 can be used as a tracer in Parkinson's disease.

Cy3 labled Inotersen sodium is a Cy3 labled Inotersen sodium.

WrFr-OCH3 is a competitive nAChR inhibitor, with IC₅₀ values of 291.9 nM, 25.3 nM, 477.5 nM and 36.5 nM against hα1β1εδ nAChR, hα9α10 nAChR, hα7 nAChR and hα9 nAChR, respectively. WrFr-OCH3 exhibits analgesic and muscle relaxant effects, reduces forelimb grip strength in rats, and alleviates Oxaliplatin (HY-17371)-induced cold allodynia in rats. WrFr-OCH3 can be used in studies related to cold allodynia.

UH 301 hydrochloride is a 5-HT_1A receptor antagonist. UH 301 hydrochloride modulates consolidation of learning in normal and cognitively impaired rats. UH 301 hydrochloride can be used for Alzheimer’s disease and amnesia research.

BChE-IN-46 is a selective and brain-penetrant BChE inhibitor (eqBChE IC₅₀ = 7.44 × 10⁻⁵ μM, SI > 270,000; hBChE, IC₅₀ = 1.48 × 10⁻³ μM). BChE-IN-46 has COX-2 inhibitory activity (IC₅₀ = 0.11 μM). BChE-IN-46 exhibits neuroprotective effects, enhances acetylcholine levels, and alleviates cognitive deficits, anxiety, and learning/memory impairments. BChE-IN-46 can be used for the development of anti-Alzheimer's disease drugs.

5-HT2CR modulator 1 (Compound 3B) is a selective, positive ago-allosteric modulator of 5HT_2CR with an EC₅₀ of 8 nM. 5-HT2CR modulator 1 is also a selective 5HT_2CR agonist with an EC₅₀ of 25 nM. 5-HT2CR modulator 1 reduces food intake.

HW161023 (compound 5) is an orally active AP2-associated protein kinase 1 (AAK1) inhibitor with IC₅₀ values of 5.4 nM and 11.9 μM aganist of AAK1and hERG, respectively. HW161023 inhibits the pain in chronic constriction injury of the sciatic nerve rat model.

Benzethonium-d7 chloride is the deuterium labeled Benzethonium chloride. Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.

Valorphin is an endogenous hemoglobin β-chain (33-39) fragment with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC₅₀ of 14 nM; Valorphin also shows anti-tumor activity.

SSR-241586 is an antagonist of neurokinin receptors. SSR-241586 is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS).

Amyloid-β-IN-1 (compound 13) is a synthetic peptide containing the hydrophobic C-terminal region "VVIA-NH2" and its reverse sequence "AIVV-NH2" of Aβ₄₂, which is an Aβ inhibitor. Amyloid-β-IN-1 can inhibit Aβ aggregation and has neuroprotective effects.

Perfluoroenanthic acid-¹³C₄ (Perfluoroheptanoic acid-¹³C₄) is the ¹³C-labeled Perfluoroenanthic acid (HY-21197). Perfluoroenanthic acid (Perfluoroheptanoic acid) is a kind of perfluoroalkyl carboxylic acid organic pollutant. Perfluoroenanthic acid has environmental persistence and bioaccumulation, and exposure can occur via oral, dermal and other routes. Perfluoroenanthic acid exhibits reproductive toxicity, neurotoxicity, hepatotoxicity, immunotoxicity and endocrine-disrupting effects. Perfluoroenanthic acid exerts definite adverse effects on development, spermatogenesis, neuronal activity and liver tissue.

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.

Bencycloquidium bromide, a muscarinic M(3) receptor antagonist, is an anticholinergic compound that acts as an anticholinergic bronchodilator. Bencycloquidium bromide can be used in the study for rhinitis.

NEK7 degrader-4 is a NEK7 molecular glue degrader with a DC₅₀ of 9  nM. NEK7 degrader-4 can be used for autoinflammatory and autoimmune disorders like multiple sclerosis, neurodegeneraive diseases like Alzheimer's disease and cardiovascular and melabolic disorders like pericarditis and Type 2 diabetes research.