801-d

Epinastine hydrochloride (WAL-801CL HCl) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.

Bicyclol (SY801)(SY 801) is an anti-hepatitis drug. Oral administration of bicyclol normalizes the elevated serum transaminases (ALT, AST) by 50% in chronic viral hepatitis B and C, and also has a certain level of inhibiting HBV and HCV replication. In combination therapy of bicyclol with interferon alpha, lamivudine and adefovir dipivoxil in HBV or HCV, bicyclol may reduce YMDD mutant and side effects and increase the anti-viral efficacy.

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

Etifoxine hydrochloride (HOE 36-801 hydrochloride) is an anxiolytic and anticonvulsant drug. Unlike benzodiazepines, Etifoxine hydrochloride appears to produce its anxiolytic effects by binding to β2 and β3 subunits of the GABAA receptor complex, and so is acting at a different target site to benzodiazepines, although the physiological effect that is produced is similar to that of benzodiazepines.

Sari 59-801 is a novel, orally effective hypoglycemic compound.

CDC801 is an inhibitor of PDE4 and TNF-α with IC50s of 1.1 μM and 2.5 μM, respectively.

Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. GABAA receptor Etifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration. Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons.

ALZ-801 is an orally available, valine-conjugated prodrug of tramiprosate. ALZ-801 is an advanced and markedly improved candidate for the treatment of Alzheimer's disease. ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, a valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound.

CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activity.CBS9106 inhibits CRM1-dependent nuclear export and reduces CRM1 protein levels.CBS9106 inhibits tumor growth and prolongs the survival of mice bearing tumor xenografts.CBS9106 is an inhibitor of CRM1-dependent nuclear export and reduces CRM1 protein levels.

5-HT2A 5-HT2C inverse agonist 1 serves as a dual and potent inverse agonist for the 5-HT2A and 5-HT2C receptors, with hERG inhibition properties that mitigate cardiovascular risks. Demonstrating significant antipsychotic efficacy in the MK-801-induced mouse model, this compound holds potential for psychosis research.

PARP1 BRD4-IN-3 (compound HF4) is an effective inhibitor of BRD4 and PARP1, with IC50 values of 1210 nM and 2019 nM respectively. The compound exhibits antiproliferative activity, induces apoptosis (apoptosis) and cell cycle arrest at the G0 G1 phase. Additionally, PARP1 BRD4-IN-3 causes DNA damage and reduces the expression of the Rad51 protein, demonstrating anti-tumor activity.

VU6024578 (BI02982816) is an orally bioavailable and selective positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGluR1. It demonstrates activation with EC50 values of 54 nM for human mGluR1 and 46 nM for rat mGluR1. VU6024578 shows antipsychotic activity in rat models of amphetamine-induced hyperactivity and MK-801-induced novel object recognition (NOR). Additionally, it possesses blood-brain barrier permeability.

VU6033685 is an orally effective positive allosteric modulator (PAM) of mGlu1, capable of positively modulating human mGlu1 and mGlu5, with EC50 values of 39 nM and 3960 nM, respectively. Additionally, VU6033685 inhibits CYP1A2, CYP2C9, and CYP2D6 with IC50 values of 26, 22.3, and 23.8 μM. It reverses amphetamine-induced hyperactivity in rats and protects against MK-801-induced cognitive deficits. VU6033685 demonstrates favorable pharmacokinetic properties in rats, with an oral bioavailability of 42.8%.

ONO-TR-772 (VU6018042) is a selective TREK inhibitor with an IC50 of 15 nM. It improves recognition memory in the NOR mouse model induced by MK-801. ONO-TR-772 is useful in research on diseases associated with cognitive impairment.

ZH8965 is an orally active TAAR1-Gs/Gq agonist (EC50: 6.1/14.8 nM) that shows efficacy in alleviating antipsychotic-like phenotypes and cognitive deficits in an MK-801-induced psychosis model in mice. It is applicable for research related to schizophrenia.

ATL-801 is anselective antagonist of A2B receptor with herapeutic activity for colitis.

NaV1.7 Blocker-801 is a potent NaV1.7 blocker.

Dizocilpine Maleate (MK-801 maleate) is a potent, selective, and non-competitive NMDA receptor antagonist with a Kd value of 37.2 nM. It is commonly used in the treatment of various neurodegenerative diseases in which NMDA receptors may be involved, and can also be used to induce schizophrenia models.

(R)-Posenacaftor ((R)-PTI-801) sodium, the R enantiomer of Posenacaftor, is a cystic fibrosis transmembrane regulator (CFTR) protein modulator. It corrects the folding and trafficking of the CFTR protein, and is utilized in the research of cystic fibrosis (CF)[1].

6,9-Dichloro-1,2,3,4-tetrahydroacridine is a synthetic intermediate in the synthesis of tacrine-based acetylcholinesterase (AChE) inhibitors.1It is also an intermediate in the synthesis of multifunctional tacrine hybrids that possess radical scavenging, amyloid-β aggregation inhibitory, and/or β-secretase 1 (BACE1) inhibitory activities in addition to their activity as AChE inhibitors.2,3 1.Recanatini, M., Cavalli, A., Belluti, F., et al.SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: Synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analoguesJ. Med. Chem.43(10)2007-2018(2000) 2.Digiacomo, M., Chen, Z., Wang, S., et al.Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of ADBioorg. Med. Chem. Lett.25(4)807-810(2015) 3.Li, S.Y., Jiang, N., Xie, S.S., et al.Design, synthesis and evaluation of novel tacrine-rhein hybrids as multifunctional agents for the treatment of Alzheimer's diseaseOrg. Biomol. Chem.12(5)801-814(2014)

Posenacaftor (PTI-801) sodium, a cystic fibrosis transmembrane regulator (CFTR) modulator, corrects CFTR protein folding and trafficking. It is utilized in researching cystic fibrosis (CF)[1].

N-(4-Aminobenzoyl)-L-glutamic acid is an oxidation product and a metabolite of tetrahydrofolate.1Levels of N-(4-aminobenzoyl)-L-glutamic acid are increased in the plasma of mice fed a high folic acid-containing diet.2 1.Reed, L.S., and Archer, M.C.Oxidation of tetrahydrofolic acid by airJ. Agric. Food Chem.28(4)801-805(1980) 2.Burton, M.A., Antoun, E., Penailillo, R.S., et al.Folic acid induces intake-related changes in the mammary tissue transcriptome of C57BL/6 miceNutrients12(9)2821(2020)

Epinastine (WAL801) is a selective and orally active histamine H1 receptor antagonist primarily used for treating allergic conjunctivitis. Epinastine also inhibits the release of IL-8 from human eosinophils and acts as a mast cell stabiliser to prevent the release of histamine.

Dizocilpine (MK-801) is a selective non-competitive NMDA receptor antagonist with a Kd of 37.2 nM that exhibits anticonvulsant effects. It acts by binding to a site within the NMDA-associated ion channel, blocking the flow of Ca²⁺, and is commonly used to establish schizophrenia models.