Neurological Disease

Cavα2δ1&NET-IN-3 (example 216) is an inhibitor of the subunit α2δ of voltage-gated calcium channels (VGCC) and noradrenaline transporter (NET). Cavα2δ1&NET-IN-3 has K_is of 100-500 nM for human α2δ-1 subunit of Ca_v2.2 calcium channel and NET, respectively.

LY302148 is a receptor ligand for 5-HT_1F. Compared to the E_max of 5-HT, LY302148 behaves as a partial agonist for the 5-HT_1F receptor. In the [³⁵S]GTPγS binding assay targeting human 5-HT_1F receptors, LY302148 exhibits good potency with an EC₅₀ value of 5.23 nM. LY302148 can be used in the research of migraine.

BIIE-0246 dihydrochloride (AR-H 053591 dihydrochloride) is a potent and highly selective non-peptide neuropeptide Y (NPY) Y₂ receptor antagonist, with an IC₅₀ value of 15 nM.

RS-102221 is a selective 5-HT2C receptor antagonist (K_i=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats.

Oxcarbazepine-d₄-1 is deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines. Anti-cancer and anticonvulsant effects.

UNC9975 is a D₂R agonist that displays signaling bias via β-arrestin–ergic signaling and a simultaneously antagonist of Gi-regulated cAMP production and partial agonist for D₂R/β-arrestin-2 interactions. UNC9975 can be utilized in antipsychotic research.

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.

Linarin (Standard) is the analytical standard of Linarin. This product is intended for research and analytical applications. Linarin (Buddleoside) is an orally active and selective inhibitor of acetylcholinesterase (AChE). Linarin has many activities, such as anti-inflammatory, antioxidant, sleep aid and sedation, bone differentiation, anti-tumor, antibacterial and antiviral. Linarin can be used to study diseases such as the nervous system, osteoporosis and cancer.

L-659837 is a NK2 receptor antagonist, and can antagonize GR 64349 (HY-P1278)-induced contraction. L-659837 can be used for study of urinary bladder disorders.

RS-64459-193 is a 5-HT1A receptor partial agonist with a K_i of 24.9 nM. RS-64459-193 also shows high affinity for 5-HT2C, 5-HT2A and 5-HT7 with pK_i values of 6.87, 7.02, and 7.18, respectively. RS-64459-193 is almost devoid of activity at the m 5-HT3 receptor.

Broflanilide (Standard) is the analytical standard of Broflanilide. This product is intended for research and analytical applications. Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.

Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a K_i of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD).

LMD-902, a LMD-009 (HY-121885) analog, is a CCR8 agonist with an EC₅₀ of 15  nM. LMD-902 has a superior binging capacity depending on key residues such as PheVI:16. LMD-902 can be used for inflammation diseases like bronchial asthma and central nervous system diseases like multiple sclerosis research.

S 1432 is a central nervous system depressant with anticonvulsant and muscle relaxant effects. S 1432 significantly reduces acetylcholine levels in the striatum inhibits convulsions induced by pentylenetetrazol. S 1432 can be used in the development of psychotropic drugs.

Neuroprotective agent 5 (compound 28) is a brain permeabilizing agent with anti-neuritis, anti-oxidative damage and neuroprotective effects. Neuroprotective agent 5 exhibits a potent NO inhibitory effect (EC₅₀=0.49 μM), inhibits the release of proinflammatory factors PGE2 and TNF-α, downregulates the expression of iNOS and COX-2 proteins, and promotes the polarization of BV-2 cells from the proinflammatory M1 phenotype to the anti-inflammatory M2 phenotype. In addition, Neuroprotective agent 5 can also inhibit acetylcholinesterase (AChE) activity and Aβ42 aggregation in a dose-dependent manner. Neuroprotective agent 5 can be used for the study of Alzheimer's disease.

SG-210 (SPR 210) is an orally active and selective aldose reductase (AR) inhibitor. SG-210 has IC₅₀ values of 9.5 nM and 10 nM for AR from porcine lens and human placenta, respectively. SG-210 can inhibit sorbitol accumulation and ameliorate diabetic neuropathy and retinopathy in Streptozotocin (HY-13753)-induced diabetic rats. SG-210 can be used in the research of diseases such as diabetes-related complications.

HSP90-IN-19 is an effective heat shock protein 90 (Hsp90) inhibitor. HSP90-IN-19 has effective Hsp90 inhibitory activity with an IC₅₀ value of 0.27 μM. HSP90-IN-19 can be used for the research of viral infection, neurodegenerative disease, and inflammation.

L-772405 is a selective 5-HT_1D receptor agonist with the K_i values of 318, 29 and ＞ 1000 nM aganist guinea pig 5-HT1_B receptor, guinea pig 5-HT_1D receptor and rat 5-HT rransporter, respectively. L-772405 decreases the potassium-induced outflow of 5-HT with an IC₅₀ value of 240 nM.

Opromazine hydrochloride is an antipsychotic medication that exhibits sedative and antiemetic pharmacological effects, making it effective for treating psychiatric disorders such as schizophrenia and psychosis. Opromazine hydrochloride functions by reducing dopaminergic activity through the blockade of dopamine receptors in the brain. Opromazine hydrochloride has been analyzed for its metabolites in various microsomal enzymes, revealing differences in formation rates that underscore the variability of drug-metabolizing enzymes in human liver and placenta microsomes.

(E)-IDO1/TDO-IN-15 is an isomer of IDO1/TDO-IN-15 (HY-184129). IDO1/TDO-IN-15 is a dual IDO1/TDO inhibitor with an IDO1 IC₅₀ of 0.19 μM and a TDO IC₅₀ of 0.37 μM. (E)-IDO1/TDO-IN-15 is applicable to the research of cancer and Alzheimer's disease.