Neurological Disease

DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB).

Casein kinase 1δ-IN-8 (compound 494) is an inhibitor of Casein kinase 1δ, Casein kinase 1δ-IN-8 can be used in the study of neurodegenerative disorders such as Alzheimer's disease.

Alimemazine-d₆ is deuterium labeled Alimemazine, which is an antihistamine.

Sphingomyelin phosphodiesterase, Bacillus cereus is a sphingomyelin hydrolase and Insecticide. Sphingomyelin phosphodiesterase, Bacillus cereus catalyzes the decomposition of sphingomyelin into ceramide and phosphorylcholine. Sphingomyelin phosphodiesterase, Bacillus cereus causes rapid paralysis and death in injected insects, including German cockroaches and black cutworms. Sphingomyelin phosphodiesterase, Bacillus cereus reduces H₂O₂ production. Sphingomyelin phosphodiesterase, Bacillus cereus can be used in studies related to sepsis and endophthalmitis.

Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease.

EMD386088 is a potent and selective 5-HT6 receptor (5-HT6R) agonist with an EC₅₀ of 1.0 nM. EMD-386088 is inactive against other HT receptors except 5-HT3R (IC₅₀ of 34 nM). EMD386088 regulates the activity of ERK1/2. EMD386088 has the potential for the research of alzheimer's disease (AD) and schizophrenia.

VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC₅₀ of 4.6 μM.

Valrocemide (TV1901) is a promising antiepileptic agent candidate that shows a broad spectrum of anticonvulsant activity.

Docosatetraenylethanolamide (DEA) is a cannabinoid receptor 1 (CB1) agonist. Docosatetraenylethanolamide inhibits the specific binding of cannabinoid probe to rat synaptosomal membranes with a K_i value of 34.4 nM. Docosatetraenylethanolamide can be used in the research of nervous system.

Nepafenac-d₅ (AHR-9434-d₅; AL-6515-d₅) is the deuterium labeled Nepafenac (HY-17357). Nepafenac, a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC₅₀ of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC₅₀ = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE_₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.

Dicarbine dihydrochloride blocks dopamine receptors in various brain parts and prevents the depression of the conditioned defence reflexes caused by stimulation of the mesencephalic portion of the reticular formation. Dicarbine dihydrochloride could be used in the schizophrenia and alcoholic psychosis studies.

NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding K_i values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.

EGLU ((2S)-α-Ethylglutamic acid; (2S)-α-EGLU) is a potent and competitive mGluR-2 receptor antagonist. EGLU interacts with (lS,3S)-ACPD-sensitive site with a K_d value of 66 μM. EGLU is an antidepressant agent.

Acacetin (Standard) is the analytical standard of Acacetin. This product is intended for research and analytical applications. Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research.

Phrixotoxin 1, from the venom of the theraphosid spider Phrixotrichus auratus, is a specific peptide inhibitor of Kv4 potassium channel.

NS1652 is a reversible anion conductance inhibitor, blocks chloride channel, with an IC₅₀ of 1.6 μM in human and mouse red blood cells.

TBTDC is a highly efficient multifunctional organic photosensitizer with aggregation-induced emission for in vivo bioimaging and photodynamic research.

Landipirdine (RO5025181; SYN120) is an orally active 5-HT6 and 5-HT2A receptors antagonist. Landipirdine can be used for the study of Parkinson disease.

Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC₅₀=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine can be used in opioid-induced constipation (OIC) research. Naldemedine is predicted to bind to 3CL^pro encoded by SARS-CoV2 genome.

R(+)-8-OH-DPAT ((R)-8-Hydroxy-2-dipropylaminotetralin) hydrobromide is a potent 5-HT_1A agonist. R(+)-8-OH-DPAT potentiates SUL (HY-B1059)-induced dopamine (DA) release in the medial prefrontal cortex (mPFC).