Neurological Disease

VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC₅₀ value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity.

YM-244769 hydrochloride (Standard) is the analytical standard of YM-244769 (hydrochloride) (HY-107659). This product is intended for research and analytical applications. YM-244769 hydrochloride is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC₅₀s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice.

Aminoquinol ((E/Z)-XIB4035) phosphate is a GFRα-1 agonist. Aminoquinol phosphate exhibits neurotrophic effects similar to GDNF and induces Ret autophosphorylation in Neuro-2A cells. Aminoquinol phosphate can be used in research related to Parkinson's disease.

(±)-Darifenacin N-Oxide is the impurity of Darifenacin (HY-A0033). Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pK_i of 8.9.

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.

Omberacetam (Standard) is the analytical standard of Omberacetam. This product is intended for research and analytical applications. Omberacetam (GVS-111) is a medication promoted and prescribed in Russia and neighbouring countries as a nootropic.

CA-074 (Standard) is the analytical standard of CA-074 (HY-103350). This product is intended for research and analytical applications. CA-074 is a potent inhibitor of cathepsin B with a K_i of 2 to 5 nM.

Eurystatin B is a prolyl endopeptidase (PED) inhibitor. Eurystatin B has a protective effect during Scopolamine (HY-N0296)-induced amnesia in rats.

Sp-8-pCPT-cGMPS is a potent cyclic guanosine monophosphate-gated channel agonist and a lipophilic activator of protein kinase G (types I α, I β, and II) and protein kinase A type II with excellent cell membrane permeability and phosphodiesterase stability. Sp-8-pCPT-cGMPS can be used to study the role of cGMP in neural plasticity and synaptic transmission.

Bisindolylmaleimide VII is a potent inhibitor of calmodulin with high affinity for calmodulin (K_d=186.2 nM). Bisindolylmaleimide VII is used to study the role of calmodulin in cancer, neurodegenerative diseases, and muscle dysfunction.

N-Demethyl amiton oxalic is an irreversible cholinesterase (ChE) inhibitor. N-Demethyl amiton oxalic elicits low-level postganglionic neuronal firing in cat vesical parasympathetic ganglia by preventing the breakdown of endogenously released ChE. N-Demethyl amiton oxalic inhibits ChE activity in squid optic ganglia and induces hyperactivity, ink ejection, pigment changes, and death, with a rate of enzymatic detoxification much lower than that of DFP. N-Demethyl amiton oxalic can be used in studies related to the mechanisms of cholinergic transmission in parasympathetic ganglia and neurotoxicology.

Imipramine-d4-1 is the deuterium labeled Imipramine (HY-W010179). Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC₅₀ value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects.

Alirinetide (Standard) (GM604 (Standard)) is the analytical standard of Alirinetide (HY-107130). This product is intended for research and analytical applications. Alirinetide (GM604) is an oligopeptide containing 6 amino acids. Alirinetide can cross the blood-brain barrier and can be used for the research of multiple neurodegenerative diseases.

6,7-Dimethylisatin (compound 1l), an Isatin (HY-Y0265) analogue, is a potent MAO inhibitor with IC₅₀s of 20.3 μM and 6.74 μM for MAO-A and MAO-B, respectively. 6,7-Dimethylisatin has the potential for depression, Alzheimer's disease and Parkinson's disease research.

Zervimesine (Standard) is the analytical standard of Zervimesine (HY-111669). This product is intended for research and analytical applications. Zervimesine (CT1812) is an orally active and brain penetrant sigma-2 receptor antagonist with a K_i of 8.5 nM. Zervimesine can be used for the research of Alzheimer’s disease.

Ambroxol (Standard) is the analytical standard of Ambroxol. This product is intended for research and analytical applications. Ambroxol (NA-872), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research.

N-Methylphenethylamine (NMPEA) hydrochloride is a potent TAAR1 agonist. N-Methylphenethylamine hydrochloride also is a trace amine neuromodulator.

RX 801077 (hydrochloride) (Standard) is the analytical standard of RX 801077 (hydrochloride) (HY-100904). This product is intended for research and analytical applications. RX 801077 hydrochloride (2 BFI) is a selective imidazoline I2 receptor (I2R) agonist with a Ki value of 70.1 nM. RX 801077 hydrochlorideshows anti-inflammation and neuroprotection. RX 801077 hydrochloride has the potential for the research of traumatic brain injury (TBI).

Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [³⁵S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.

Desmethylmoramide is structurally similar to known opioids. Desmethylmoramide has analgesic activity in rodents.