pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
BF 227 is a candidate for an amyloid imaging probe for PET, with a Ki of 4.3 nM for Aβ1-42 fibrils.
Frentizole, an FDA-approved immunosuppressive drug, is a novel inhibitor of the Aβ-ABAD interaction.IC50 value:Target: Aβ-ABAD interaction
Ginsenoside Rg3 is the main component of Red ginseng. Ginsenoside Rg3 inhibits Na+ and hKv1.4 channel with IC50s of 32.2±4.5 and 32.6±2.2 μM, respectively. Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.
Colivelin is a neuroprotective peptide and activator of STAT3.
Amyloid β-Protein (10-20) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.
β-Amyloid (1-15) is a fragment of β-Amyloid peptide. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
β-Amyloid (1-28) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
β-Amyloid (1-16) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
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.
MK-3328 is a β-Amyloid PET ligand, which exhibits high binding potency with an IC50 of 10.5 nM.
Amyloid β-Peptide (1-42) human is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.
Schisantherin B is a natural product.
β-amyloid (1-11) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.
β-amyloid (12-28) is a 17-aa peptide fragment, which can produce amyloid aggregates, used in the research of Alzheimer’sdisease.
DWK-1339 is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.
β-Amyloid (29-40) is a fragment of Amyloid-β peptide.
gamma-Secretase Modulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor. gamma-Secretase Modulators is useful for Alzheimer's disease.IC50 value:Target: γ-secretase modulator
Semagacestat is a γ-secretase inhibitor, inhibits β-amyloid (Aβ42), Aβ38 and Aβ40 with IC50 of 10.9, 12 and 12.1 nM, respectively; also inhibits Notch signaling with IC50 of 14.1 nM.
Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 acts as a NF-κB inhibitor. Ginsenoside Rg2 also reduces Aβ1-42 accumulation.
Tramiprosate is a small, orally-administered compound that binds to soluble Aβ and reduces amyloid aggregation and subsequent depositiontarget: AβIn vitro: Tramiprosate provides neuroprotection against Aβ-induced neurotoxicity in neuronal and mouse organotypic hippocampal cultures, and reverses Aβ-induced long-term potentiation (LTP) inhibition in rat hippocampus, in part, through activation of β-aminobutyric acid A (GABA-A) receptors. Tramiprosate dose-dependently provides neuroprotection against ischemic stroke.In vivo: Tramiprosate produced dose-dependent reductions of Aβ in the brain of transgenic mice (hAPP-TgCRND8). Clinical studies show that tramiprosate was safe and tolerable. In mild-to-moderate AD patients tramiprosate also reduced Aβ42 levels in CSF.The reference for animal administration is 50 mg/kg.
ARN2966 is a potent post-transcriptional modulator of APP expression; reduces expression of APP with resultant lower production of Aβ. IC50 value: Target: AβThis potent post-transcriptional modulation of APP expression differs from other mechanisms such as inhibition of secretases. Secretase inhibitors have been pursued as disease modifying strategies by a number of pharmaceutical firms but they have encountered numerous setbacks during clinical development. ARN2966 is non toxic, orally absorbable, blood-brain-barrier penetrable, and effective in vitro and in vivo.
Deferoxamine mesylate is an iron chelator that binds free iron in a stable complex, preventing it from engaging in chemical reactions.
Edonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ).
β-Amyloid (1-42), rat is a 42-aa peptide, shows cytotoxic effect on acute hippocampal slices, and used in the research of Alzheimer's disease.
Geniposide is an iridoid glucoside extracted from Gardenia jasminoides Ellis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.
β-Amyloid (10-35), amide is composed of 26 aa (10-35 residues of the Aβ peptide) and is the primary component of the amyloid plaques of Alzheimer’s disease.
K 01-162 (K162) binds and destabilizes AβO (β-amyloid), with an EC50 of 80 nM. IC50 value: 80 nM (EC50)Target: Amyloid-βin vitro: The active drug candidate K162 (EC50 = 0.080 μM), stabilizes hydrophobic core I of Aβ42 peptide (residues 17-21) to its α-helical conformation by interacting specifically in this region. [1] K01-162 shows full MC65 protection at 125 nM, an EC50 of 80 nM, and no cytotoxicity up to 50 μM. [2]in vivo：K01-162 can reduce the brain amyloid burden that exists in both fibrillar and RIPA-soluble, non-fibrillar forms.[2]
Notoginsenoside R1, the main bioactive component in panaxnotoginseng, is reported to have some neuronal protective, antihypertensive effects. IC50 value:Target:In vitro:In vivo: Notoginsenoside R1 significantly reduce blood pressure in spontaneously hypertensive rats and induce nitric oxide generation through increasing the phosphorylation of iNOS. Notoginsenoside R1 reduces the caudal blood pressure of spontaneously hypertensive rats through induction of iNOS regulated by long non-coding RNA AK094457 [1]. The mice with notoginsenoside R1 treatment showed significant amelioration in the cognitive function and increased choline acetyl transferase expression, as compared to the vehicle treated mice. Notoginsenoside R1 treatment inhibited Aβ accumulation and increased insulin degrading enzyme expression in both APP/PS1 mice and N2a-APP695sw cells [2]. In Notoginsenoside R1 treated rats, expression of TGF-β1and Smad3 at each time point was down-regulated, with statistical significance(P0.05) compared with that in the NDMA group [3].
Ginsenoside Rg1 is one of the major active components of ginseng. Ginsenoside Rg1 displays promising effects by reducing cerebral Aβ levels. Ginsenoside Rg1 also reduces NF-κB nuclear translocation.