γ-secretase Modulator

Bepridil hydrochloride (CERM 1978; Org 5730 hydrochloride) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil hydrochloride acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

Bepridil hydrochloride hydrate (CERM 1978 hydrate; Org 5730 hydrochloride hydrate) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride hydrate modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil hydrochloride hydrate acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride hydrate alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride hydrate also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride hydrate is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

Bepridil (CERM 1978 (free base); Org 5730) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.

PF-06648671 is a novel, brain-penetrable, and orally active γ-secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.

JNJ-40418677 is an orally active modulator of γ-secretase, can cross the blood-brain barrier. JNJ-40418677 inhibits Aβ42 and NS2B-NS3 protease, with IC₅₀s of 200 nM and 3.9 μM, respectively. JNJ-40418677 displays good biological tolerance, can be use for Alzheimer’s disease research.

(E/Z)-Sulindac sulfide is a potent γ-secretase modulator (GSM). (E/Z)-Sulindac sulfide selectively reduces Aβ42 production in favor of shorter Aβ species. (E/Z)-Sulindac sulfide can be used for researching Alzheimer’s disease.

RO7185876 is a potent and selective gamma secretase modulator as a potential research for Alzheimer's disease.

gamma-secretase modulator 6 (Example 50) is a gamma-secretase modulator. gamma-secretase modulator 6 inhibits Aβ42 secretion in HEK cell line stably expressing APP (Aβ amyloid precursor protein) (pIC₅₀: 8.1). gamma-secretase modulator 6 can be used for research of Alzheimer's disease.

NGP555 is a γ-secretase modulator. NGP555 Lowers the Amyloid Biomarker Aβ42.

FRM-024 is a central nervous system-penetrant, orally active γ-secretase modulator and Aβ42 lowering agent. FRM-024 is used for the research of familial Alzheimer's disease.

GSM III is a γ-Secretase complexe (GSEC) modulator. GSM III significantly regulates amyloid-β (Aβ) length at the extracellular interface between the protease (NCT, PSEN) and the substrate APP_C99. GSM III can be used for Alzheimer's disease (AD) research.

GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1).

(-)-FRM-024 is the (-)-isomer of FRM-024, a potent CNS-penetrant gamma secretase modulator that can be utilized in Alzheimer’s disease research.

Nivegacetor (RG6289) a potent and selective γ-secretase modulator. Nivegacetor can reduce the production of Aβ42 can be used for the research of Alzheimer's disease.

BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC₅₀ values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.

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

gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for study of Alzheimer's disease.

gamma-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.

Gamma-secretase modulator 3 is a γ-secretase modulator. Gamma-secretase modulator 3 has the potential for use in research on neurological diseases such as Alzheimer's disease.