Neurological Disease

Sacubitrilat-¹³C₄ (Desethyl Sacubitril-¹³C₄) is ¹³C labeled Sacubitrilat. Sacubitrilat (Desethyl Sacubitril) is an active neprilysin (NEP) inhibitor.

18-Methoxycoronaridine ((-)-18-Methoxycoronaridine) is an orally active and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist. 18-Methoxycoronaridine is an inhibitor of serotonin transporter (SERT) and norepinephrine transporter (NET), with IC₅₀ values of 51.6 μM and 121 μM for SERT and NET, respectively. 18-Methoxycoronaridine inhibits the function of SERT and NET, promotes 5-HT3A receptor desensitization, blocks α3β4 nAChR, and modulates receptor signaling pathways associated with reinforcement. 18-Methoxycoronaridine also exhibits potent antiparasitic activity. 18-Methoxycoronaridine can be used in research related to depression, obesity, alcoholism, smoking addiction, and cutaneous leishmaniasis.

CTPI-2 (Standard) is the analytical standard of CTPI-2 (HY-123986). This product is intended for research and analytical applications. CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a K_D of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet. Antitumor activity.

Tamolarizine hydrochloride is a calcium channel blocker. Tamolarizine hydrochloride crosses the blood-brain barrier and antagonizes the effects of calcium on neurons. Tamolarizine hydrochloride can be used in nervous system research.

Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC₅₀ values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC₅₀s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease. Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC₅₀ of 3.5 μM, can be used for the research of metabolic disorders.

IDO-IN-19 (Compound I) is a free base of an imidazole-isoindole derivative. IDO-IN-19 can inhibit the activity of Indoleamine 2,3-Dioxygenase (IDO). IDO-IN-19 can block the decomposition of tryptophan and restore the function of T cells. IDO-IN-19 can be used for the researches of cancer, immunology, infection and neurological disease, such as breast cancer and Alzheimer's disease.

Neuroprotectin B is a cyclopeptide. Neuroprotectin B has the function of protecting chicken brain neuron culture from excitatory toxicity induced by glutamate and red alginate.

Bepridil hydrochloride (Standard) (CERM 1978 (Standard);Org 5730 hydrochloride (Standard)) is the analytical standard of Bepridil hydrochloride (HY-103315). This product is intended for research and analytical applications. Bepridil hydrochloride is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil hydrochloride acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

DL-AP5 (sodium) (Standard) is the analytical standard of DL-AP5 (sodium). This product is intended for research and analytical applications. DL-AP5 (2-APV) sodium is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 sodium shows significantly antinociceptive activity. DL-AP5 sodium specifically blocks on channels in the rabbit retina.

ZINC12613047 is a selective BChE inhibitor with an IC₅₀ of 0.021 μM against huBChE. ZINC12613047 can be used for the research of Alzheimer's disease.

LY231617 (Standard) is the analytical standard of LY231617 (HY-103253). This product is intended for research and analytical applications. LY231617 is a potent and blood-brain barrier penetrable antioxidant. LY231617 is a neuroprotective agent in brain, it can be used for the research of nervous disease.

SB-408124 (Hydrochloride) (Standard) is the analytical standard of SB-408124 (Hydrochloride). This product is intended for research and analytical applications. SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor.

Tianeptine sodium salt (Standard) is the analytical standard of Tianeptine sodium salt (HY-90003A). This product is intended for research and analytical applications. Tianeptine sodium salt is an atypical antidepressant. Tianeptine sodium salt is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine sodium salt is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine sodium salt increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine sodium salt exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine sodium salt inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine sodium salt can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.

Enciprazine is an orally active non-benzodiazepine anxiolytic. Enciprazine acts as an agonist of 5-HT₁A receptor (5-HT₁AR) and an antagonist of α₁-adrenergic receptor (α1-adrenergic receptor) . Enciprazine induces drug-related electroencephalogram changes by reducing the average power of δ waves and θ waves, and increasing the average power of α waves and fast β waves. Enciprazine exhibits anti-aggressive activity, with only weak sedative and ataxic effects. Enciprazine regulates plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis. Enciprazine can be used in research related to anxiety disorders, generalized anxiety syndrome and psychosis.

NUCC-390 dihydrochloride (Standard) is the analytical standard of NUCC-390 (dihydrochloride) (HY-111793A). This product is intended for research and analytical applications. NUCC-390 dihydrochloride is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 dihydrochloride induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 dihydrochloride promotes nerve recovery of function after neurodegeneration in vivo.

CUMI-101 (compound 8) is a 5-HT_1AR agonist (K_i=0.15 nM) with an EC₅₀ of 0.1 nM in the [35S]GTPγS binding assay. CUMI-101 can be used in the research of neurological diseases.

M 16287 is an orally active aldose reductase inhibitor, with an IC₅₀ of 0.08 μM in rats and 0.25 μM in cattle. M 16287 improves lens fiber swelling and vacuolization, prevents galactitol accumulation, delays inositol depletion, inhibits glutathione reduction, restores the NADPH/NADP⁺ ratio to normal, and normalizes lens Na⁺ content and Na⁺/K⁺ ratio. M 16287 prevents galactose-induced cataract formation in rats. M 16287 improves motor nerve conduction velocity in diabetic rats, partially alleviates histopathological changes in the sciatic nerve, and inhibits sorbitol accumulation. M 16287 can be used in studies related to cataracts and diabetic neuropathy.

Proglumide (sodium) (Standard) is the analytical standard of Proglumide (sodium). This product is intended for research and analytical applications. Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities.

JNJ-10258859 is a potent and selective phosphodiesterase type 5 inhibitor, with a K_i of 0.23 nM. JNJ-10258859 can be used for erectile dysfunction research.

GW 833972A (Standard) is the analytical standard of GW 833972A (HY-101765). This product is intended for research and analytical applications. GW 833972A is a selective CB₂ receptor agonist with pEC₅₀ of the human CB₂ receptor for GW 833972A of 7.3, and its selectivity for the CB₂ receptor is approximately 1000 times higher than that for the CB₁ receptor. GW 833972A inhibits induced neuronal depolarization and suppresses coughing caused by citric acid in guinea pig models. GW 833972A can be used for the study of chronic cough.