Beta-secretase Inhibitor

BACE1-IN-1 (Standard) is the analytical standard of BACE1-IN-1 (HY-100182). This product is intended for research and analytical applications. BACE1-IN-1 is an orally active, blood-brain barrier penetrant dual-target inhibitor of BACE1/2, with IC₅₀ values of 23 nM and 24 nM against human BACE1 and BACE2, respectively. BACE1-IN-1 reduces cerebral Aβ40 levels in mice. BACE1-IN-1 can be used in studies related to Alzheimer's disease and type 2 diabetes.

Aloenin (Standard) is the analytical standard of Aloenin. This product is intended for research and analytical applications. Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitory activity on β-secretion (BACE) (IC₅₀=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release.

Bepridil hydrochloride (Standard) (CERM 1978 (Standard);Org 5730 hydrochloride (Standard)) is the analytical standard of Bepridil hydrochloride (HY-103315). This product is intended for research and analytical applications. Bepridil 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.

Dehydroevodiamine hydrochloride Standard is the analytical standard of Dehydroevodiamine hydrochloride (HY-N6029). This product is intended for research and analytical applications. Dehydroevodiamine hydrochloride is a blood-brain barrier-permeable, orally effective AChE and BACE1 inhibitor (IC₅₀ = 40.96 μM). Dehydroevodiamine hydrochloride is isolated and extracted from Evodia rutaecarpa. Dehydroevodiamine hydrochloride attenuates neurotoxicity through multiple targets by inhibiting BACE1 to block Aβ production, inhibiting AChE activity, scavenging ROS, and suppressing calcium influx. Dehydroevodiamine hydrochloride can be used for research on Alzheimer's disease, cerebral ischemia, vascular dementia, and other cognitive disorder-related diseases.

(1α,1'S,4β)-Lanabecestat (Standard) is the analytical standard of (1α,1'S,4β)-Lanabecestat (HY-100740C). This product is intended for research and analytical applications. (1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.

Bepridil-d₅ hydrochloride (CERM 1978-d₅; Org 5730-d₅ hydrochloride) is the deuterated-labeled Bepridil hydrochloride (HY-103315). 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.

(S)-(-)-Anatabine is an NFκB/BACE-1 inhibitor with blood-brain barrier penetration. (S)-(-)-Anatabine inhibits NFκB activation via phosphorylation of its p65 subunit. (S)-(-)-Anatabine inhibits BACE-1 transcription and reduces BACE-1 protein levels. (S)-(-)-Anatabine lowers production of Aβ_1-40 and Aβ_1-42 by reducing β-cleavage of amyloid precursor protein without affecting α-cleavage. (S)-(-)-Anatabine can be used for the research of Alzheimer's disease.

TB-11 is a Cathepsin D inhibitor, with IC₅₀s of 0.126 nM (Cathepsin D), 1.92 nM (Cathepsin E), 48.8 nM (BACE1), respectively. TB-11 can be used for tumor research.

WJM590 is an orally active antimalarial agent that also exhibits inhibitory activities against renin, cathepsin D, BACE1, and plasmodial aspartic proteases. WJM590 inhibits substrate and protein maturation processing mediated by key proteases of Plasmodium falciparum, arrests asexual blood-stage parasites at the late schizont stage, inhibits merozoite release, and blocks malaria parasite transmission via vectors. WJM590 exerts selective inhibitory activity against multiple Plasmodium species and drug-resistant Plasmodium falciparum strains, and reduces parasitemia in infected mice. WJM590 can be used in malaria-related research.

Umibecestat hydrochloride (CNP520 hydrochloride) is a selective, orally active BACE inhibitor, with an IC₅₀ of 11 nM for hBACE-1, 10 nM for mouse BACE-1, and 30 nM for hBACE-2. Umibecestat hydrochloride reduces β-Amyloid levels in the brain and cerebrospinal fluid, decreases β-amyloid plaque deposition, and inhibits plaque-associated neuroinflammation. Umibecestat hydrochloride is used in research related to Alzheimer's disease.

AZ-4217 is an inhibitor for β-site amyloid precursor protein cleavage enzyme 1 (BACE1), with IC₅₀ of 160 pM in human SH-SY5Y cells. AZ-4217 reduces amyloid deposition in Tg2576 mouse models, and is used for Alzheimer’s Disease research.

Verubecestat tosylate is an orally active, high-affinity BACE1 and BACE2 inhibitor with K_i values of 2.2 nM and 0.38 nM. Verubecestat tosylate effectively reduces Aβ40 and has the potential for Alzheimer's Disease.

LY2811376 (Standard) is the analytical standard of LY2811376 (HY-10472). This product is intended for research and analytical applications. LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC₅₀ of 239 nM-249 nM, that acts to decrease Aβ secretion with EC₅₀ of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.

Lanabecestat (Standard) is the analytical standard of Lanabecestat. This product is intended for research and analytical applications. Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease.

LX2343 (Standard) is the analytical standard of LX2343 (HY-111383). This product is intended for research and analytical applications. LX2343 is a BACE1 enzyme inhibitor with an IC₅₀ value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC₅₀ of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.

β-Secretase Inhibitor IV (Standard) is the analytical standard of β-Secretase Inhibitor IV (HY-10133). This product is intended for research and analytical applications. β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.

Eslicarbazepine (Standard) is the analytical standard of Eslicarbazepine. This product is intended for research and analytical applications. Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.

SEW06622 is a BACE-1 inhibitor with an IC₅₀ value of 6.3 μM and can be used in Alzheimer's disease research.

Aloeresin D (Standard) is the analytical standard of Aloeresin D. This product is intended for research and analytical applications. Aloeresin D is a chromone glycoside isolated from Aloe vera, inhibits β-Secretase (BACE1) activity, with an IC₅₀ of 39 μM.

PF-06663195 is a β-secretase (BACE1) inhibitor, with BACE1 CFA and BACE1 WCA IC₅₀ values of 53 and 15 nM, respectively. PF-06663195 can be used for Alzheimer's disease research.