gamma-secretase modulator 2

Gamma-secretase modulator 2 is a potent, selective compound for the treatment of Alzheimer's disease, specifically designed to modulate γ-secretase activity. This modulation selectively attenuates the production of Aβ(1-42), addressing diseases associated with Aβ deposition in the brain, particularly Alzheimer's disease.

CB2R/FAAH modulator-2 (compound 26) is a dual modulator targeting at CB2R and FAAH. CB2R/FAAH modulator-2 acts as a CB2R agonist and FAAH inhibitor, the Ki values are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 has studies research value related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.

γ-Secretase modulator 13 is a γ-secretase modulator (GSMs) that inhibits the production of amyloid β-peptide Aβ42 and can be used to study Alzheimer's disease and tumors.

gamma-secretase modulator 1 is a modulator of γ secretase and can be used in studies about the treatment of Alzheimer's disease.

AMPA receptor modulator-2 (Example 134) is a AMPA receptor modulator, with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor[1]. pIC50 = -lgIC50. [1]. BERRY CYNTHIA G B (US), et al. AZABENZIMIDAZOLES AND THEIR USE AS AMPA RECEPTOR MODULATORS. Patent. WO2016176460.

5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT , is a modulator of 5-HT1A with a Ki of 53 nM for 5-HT1A binding[1]. [1]. Naiman, N.,et al. 2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites. Journal of Medicinal Chemistry, 1989;32(1), 253-256.

Gamma-Glutamyl Transferase-IN-2 (compound 4dq), a β-carboline 1-hydrazide inhibitor, exhibits both antifungal and antibacterial properties by targeting glutamyltransferase. Its mode of action includes inducing reactive oxygen species accumulation, compromising cell membranes, and disrupting histone acetylation processes [1].

Anti-Mouse TCR V gamma 2 Antibody is a host Armenian Hamster-derived IgG inhibitory antibody targeting mouse TCR V gamma 2.

Sirtuin modulator 2 (N-(3-(imidazo[2,1-b]thiazol-6-yl)phenyl)-2-methoxybenzamide) exhibits antidiabetic, anti-inflammatory and antitumor activities.

DPP-4/GPR119 modulator 2 is an inhibitor of dipeptidyl peptidase IV (DPP-IV) (IC50: 0.22 μM) and an agonist of GPR119 (EC50: 0.95 μM).

γ-Secretase modulator 4 is a potent γ-secretase modulator, reduces the Aβ42 level with IC50s of 0.017 μM and 0.014 μM in mouse and human, respectively.

CXCR7 modulator 2 is a 7-type C-X-C chemokine receptor (CXCR7) modulator with a Ki of 13 nM.

Nur77 modulator 2 is a Nur77 regulator with a Kd value of 0.35 μM. Nur77 modulator 2 is also a potent, orally active inhibitor of inflammation. nur77 modulator 2 regulates Nur77 co-localization in mitochondria.

GPR120 modulator 2 is useful for modulating GPR120.

A1AT Modulator 2, an α-1 antitrypsin (A1AT) modulator, exhibits an IC50 value greater than 1.0 μM and an EC50 value less than 0.4 μM. It is utilized in the study of infection and inflammation.

IL-17A modulator-2, exhibits inhibitory properties towards IL-17A, with a pIC50 of 8.3. Its effectiveness lies in attenuating the biological effects associated with IL-17A activity. IL-17A modulator-2 finds utility in the study of diseases and disorders characterized by dysregulated IL-17A modulation, such as those involving immune dysfunction, autoimmune pathology, cancer, and neurodegenerative conditions.

γ-Secretase modulator 12 (Compound 1a) is a selective compound that effectively reduces amyloid-β42 (Aβ42) levels with an IC50 of 0.39 μM. It is specifically designed for Alzheimer's disease research. Notably, γ-Secretase modulator 12 exhibits a favorable brain/plasma ratio (Kp, brain = 0.72) in mice [1].

β-Catenin Modulator-2 (Compound IIa-130), which is an oxazole-thiazole derivative, serves as a potent and selective modulator of β-Catenin [1].

gamma-Secretase Modulators serves as a useful treatment for Alzheimer's disease by inhibiting the production of Amyloid-β. Specifically, it acts as a gamma-Secretase Modulators with an IC50 value.

PCSK9 modulator-2 (Compound 1) is a potent PCSK9 modulator (EC 50 = 202 nM) that has the potential to be used in hyperlipidemia research. Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a recently validated therapeutic target for lowering low-density lipoprotein cholesterol (LDL-C) [1].

gamma-secretase modulator 5 (compound 22d) is a gamma-secretase modulator (GSMs) that crosses the blood-brain barrier and exhibits an inhibitory effect on the production of the aggregated amyloid β peptide Aβ42 (IC50: 60 nM). gamma-secretase modulator 5 can be used in the study of Alzheimer's disease. The gamma-secretase modulator 5 can be used to study Alzheimer's disease.

NMDA receptor modulator 2 (Compound 1) is a potent modulator of the NMDA receptor that can be used for neurological disorder research [1].

CXCR4 modulator-2 (compound Z7R) is a potent modulator of CXCR4 (IC50: 1.25 nM). CXCR4 modulator-2 exhibits good stability in mouse serum (t1/2= 77.1 min) and has anti-inflammatory effects in a mouse oedema model.

γ-Secretase modulator 10 is a novel γ-secretase modulator.

nAChR modulator-2, a insecticide, is a insect nAChR orthosteric modulator [1] .

RORγt modulator 2 is a modulator of retinol-related orphan receptor γt (RORyt) (IC50<50 nM) and can be used in the study of RORγt-mediated diseases such as pain, inflammation, asthma, rheumatoid arthritis, COPD, multiple sclerosis, psoriasis, colitis, neurodegenerative diseases and cancer.

P-gp modulator 2 (Compound 27) is a potent competitive and metabotropic P-glycoprotein (P-gp) modulator.

gamma-secretase inhibitior-1 is a gamma-secretase modulator that is useful to Alzheimer's disease [1].

gamma-secretase modulator 3 is a gamma-secretase modulator.

MRGPRX4 modulator-2 is a potent modulator of Mas-related G protein receptor X4 (MRGPR X4).MRGPRX4 modulator-2 can be used to study autoimmune diseases and inflammation.

RNA splicing modulator 2 (compound 256) is a RNA splicing modulator [1] .

γ-Secretase modulator 11 hydrochloride is a potent, orally active γ-secretase modulator (IC50: 0.029 μM). γ-Secretase modulator 11 hydrochloride significantly reduces brain Aβ42 levels and rescues the cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has shown research potential in Alzheimer's disease.

KCa2 channel modulator 2 (compound 2q) is an effective subtype-selective K/Ca 2 channel positive modulator which shows similar potency on the human K Ca 2.3 channel and rat K Ca 2.2a subtypes, with EC50 values of 0.60 μM and 0.64 μM, respectively [1].

5-{8-[(3,4'-Difluoro[1,1'-biphenyl]-4-yl)methoxy]-2-methylimidazo[1,2-a]pyridin-3-yl}-N-methylpyridine-2-carboxamide (1o) exhibited high in vitro potency and brain exposure, was able to cause a significant reduction in brain Aβ42 levels, and had no inhibitory effect on cytochrome p450 enzymes. In addition, compound 1o exhibited excellent anti-cognitive deficits in AD model mice.

GABAA receptor modulator-2 (Compound 20) is a selective, orally active α5-GABAAR negative conformation modulator (Ki: 4.1 nM). gABAA receptor modulator-2 exhibits high metabolic stability and a good central nervous system safety profile.

CB1R Allosteric modulator 2 (compound 18) is a potent allosteric modulator of the CB1R receptor. It exhibits negative modulation of the functional activity of orthosteric ligands (NAM) at CB1Rs, as demonstrated in previous studies [1].

mGluR2 modulator 2 (compound 2) can be used in antipsychotic research. mGluR2 modulator 2 is a potent, selective and orally bioavailable positive allosteric modulator of mGluR2 with an EC 50 value of 0.13 μM [1].

Kv3 modulator 2 is a potent Kv3 channels modulator.has analgesic activity and is used in the prophylaxis or treatment of related disorders.