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 CB2R and FAAH, acting as a CB2R agonist (Ki = 10.8 nM) and FAAH inhibitor (IC50 = 6.2 μM), with a Ki value of 152.9 nM for CB1R. It has research value in cancer, deleterious inflammatory cascades 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 an 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.

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 that reduces Aβ42 levels with IC50s of 0.017 μM in mice and 0.014 μM in humans.

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

γ-Secretase modulator 12 (Compound 1a) is a selective compound that effectively reduces amyloid-β42 (Aβ42) levels with an IC50 of 0.39 μM, 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].

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.

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.

GPR120 modulator 2 is useful for modulating GPR120.

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.

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

Anti-Mouse TCR V gamma 2 Antibody is an inhibitory IgG antibody derived from Armenian Hamster, targeting mouse TCR V gamma 2.

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

PCSK9 modulator-2 (Compound 1) is a potent PCSK9 modulator (EC 50 = 202 nM) with potential applications 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 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.

Gamma-secretase modulator 5 (compound 22d) is a gamma-secretase modulator (GSM) that crosses the blood-brain barrier and inhibits the production of the aggregated amyloid β peptide Aβ42 (IC50: 60 nM). This compound is valuable for studying Alzheimer's disease.

NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator suitable for neurological disorder research [1].

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

γ-Secretase modulator 10 (GSM-10) is a novel compound that modulates γ-secretase activity.

nAChR modulator-2, an insecticide, functions as an orthosteric modulator of insect nAChR [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 modulator of P-glycoprotein (P-gp).

Gamma-secretase inhibitor-1 is a gamma-secretase modulator valuable for Alzheimer's disease [1].

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

CB1R Allosteric Modulator 2 (compound 18) is a potent negative allosteric modulator (NAM) of CB1R receptor activity, as demonstrated in previous studies [1].

mGluR2 modulator 2 (compound 2) is a potent, selective, and orally bioavailable positive allosteric modulator of mGluR2 with an EC50 value of 0.13 μM [1], and can be used in antipsychotic research.

Gamma-secretase modulator 3 [gamma-secretase modulator] is a compound that regulates gamma-secretase activity.

RNA splicing modulator 2 (compound 256) is an 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 with similar potency on the human K Ca 2.3 channel and rat K Ca 2.2a subtypes, exhibiting 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, significantly reduced brain Aβ42 levels, showed no inhibitory effect on cytochrome p450 enzymes, and demonstrated 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) that exhibits high metabolic stability and a good central nervous system safety profile.

MRGPRX4 modulator-2 (compound 1-55) is a highly potent antagonist of MRGPRX4 with an IC50 value of less than 100 nM. Its notable applications include research on autoimmune diseases such as psoriasis, multiple sclerosis, Steven Johnson's Syndrome, and various chronic itch conditions [1].