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Alzheimer's Disease Targeted Libraries

Alzheimer's disease targeted librariesDuring the past decades, several agents have been approved that enhance cognition of Alzheimer's disease (AD) patients. However, the effectiveness of these treatments are limited or controversial and they do not modify disease progression. Recent advances in understanding AD pathogenesis have led to the development of numerous compounds that might modify the disease process. Taking into account AD complexity, it becomes clear that polypharmacology with drugs targeting different sites could be the future treatment approach and a majority of the recent drugs under evaluation seems to act on multiple targets.

 

 
Otava offers 29 Alzheimer's disease Targeted Libraries designed with Ligand-based and Receptor-based approach. These libraries are proposed for screening in AD-associated research and drug development projects.

  • the libraries contain drug-like compounds only
  • all the compounds are in stock
  • cherry picking is available

In this collection of targeted libraries we included those activities which fall into two Alzheimer's treatment categories: (i) disease-modifying treatments that target and reduce the secondary pathologies of the disease, leading to the cessation or the reversal of disease progression; and (ii) symptomatic treatments that treat the tertiary cognitive symptoms of the disease and protect from further cognitive decline.

 

All the targeted libraries contain molecules with increased potential for CNS bioavailability. Filtering by polar surface area parameter (PSA) which discriminates CNS penetrating compounds, we selected only those compounds having increased BBB permeability. 

 

List of OTAVA's Alzheimer's disease Targeted Libraries:

You can sort data by any column and use "Filter" option to search library's name:

Name Number of compounds Approach
12 Lipoxygenase inhibitor 27 Ligand-based Ligand-based
5 Hydroxytryptamine 1A antagonist 168 Ligand-based Ligand-based
5 Hydroxytryptamine 6 antagonist 114 Ligand-based Ligand-based
Acetylcholine nicotinic agonist 186 Ligand-based Ligand-based
Acetylcholinesterase inhibitor 243 Ligand-based Ligand-based
Adenosine A1 receptor antagonist 55 Ligand-based Ligand-based
Benzodiazepine inverse agonist 35 Ligand-based Ligand-based
Beta Secretase 1 (BACE1) inhibitor 1130 Receptor-based Receptor-Based
Calcium channel antagonist 623 Ligand-based Ligand-based
Caspase 9 inhibitor 44 Ligand-based Ligand-based
Cyclin-dependent kinase 2 (CDK2) inhibitor 1292 Receptor-based Receptor-Based
Cyclin-dependent kinase 5 (CDK5) inhibitor 2230 Receptor-based Receptor-Based
Cyclooxygenase 1 inhibitor 133 Ligand-based Ligand-based
Glutamate receptor antagonist 44 Ligand-based Ligand-based
Glycogen synthase kinase-3 beta (GSK3) inhibitor 1645 Receptor-based Receptor-Based
Interleukin 1 antagonist 299 Ligand-based Ligand-based
MAO B inhibitor 126 Ligand-based Ligand-based
Mitogen Activated Protein Kinase1 (ERK2, MAPK1) inhibitor 606 Receptor-based Receptor-Based
NMDA receptor antagonist 38 Ligand-based Ligand-based
Peroxisome proliferator-activated receptor gamma agonist 127 Ligand-based Ligand-based
Protein kinase B (PKB/Akt) inhibitor 1597 Ligand-based Ligand-based
Caspase-3 inhibitor* Up to 2000 Receptor-based Receptor-Based
Dual-specificity tyrosine-phosphorylation regulated kinase 1A (DYRK1A) inhibitor* Up to 2000 Receptor-based Receptor-Based
Heat shock protein 90 (Hsp90) inhibitor* Up to 2000 Receptor-based Receptor-Based
Interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor* Up to 2000 Receptor-based Receptor-Based
c-Jun N-terminal kinase 3 (JNK3, MAPK10) inhibitor* Up to 2000 Receptor-based Receptor-Based
Microtubule-affinity regulation kinase 2 (MARK2) inhibitor* Up to 2000 Receptor-based Receptor-Based
Tumor protein 53 (p53) inhibitor* Up to 2000 Receptor-based Receptor-Based
cAMP-dependent protein kinase (PKA) inhibitor 346 Receptor-based Receptor-Based

Libraries marked by (*) can be prepared on request

 

Also, we offer bioactive compounds with known modulating activity towards molecular targets related to Alzheimer's disease:

 

Bioactive compound available Catalog number CAS number Bioactive compound description
1059264 1059264 867284-43-3 4-[1-(4-Chlorophenyl)cyclopentyl]-2-thiazolamine.
β-Secretase Inhibitor
7015070102 7015070102 211555-08-7 3-[(6,7-Dimethoxy-4-quinazolinyl)amino]-phenol (Janex 3; WHI-P180).
Potent inhibitor of IgE-mediated mast cell responses to allergens in vitro and in vivo. Also inhibits cyclin-dependent kinase 2 (CDK2; IC50 = 1µM) by blocking the ATP site
7070707001 7070707001 304913-22-2 4-Amino-N-(4-chlorophenyl)-N-methyl-benzenesulfonamide (ZXX2-77).
Benzenesulfonanilide-type cyclooxygenase-1-selective inhibitor
7114471128 7114471128 1093757-42-6 (±)-cis-2-{[(3,5-dichlorophenyl)amino]carbonyl}cyclohexanecarboxylic acid ((1R,2S)-rel-2-[[(3,5-dichlorophenyl)amino]carbonyl]-cyclohexanecarboxylic acid; VU0155041).
Positive allosteric selective modulator at mGluR4 (EC50 values are 798 nM and 693 nM at human and rat mGluR4 receptors respectively). It has advantages over PHCCC (Asc-043) as it is water soluble and more potent. Active in behavioural models of Parkinsons Disease.
7070707013 7070707013 601514-19-6 3-[[6-(3-aminophenyl)-1H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]-phenol (TWS119).
Potently inhibits GSK3β with an IC50 value of 30 nM. At 400 nM, TWS119 induces neurogenesis in murine embryonic stem cells making it a useful tool to regulate stem cell self-renewal and differentiation
7070707014 7070707014 81094-64-6 1,2-Dihydro-2-naphthalenamine hydrochloride.
Potent antagonist of the modulatory glycine site of the N-methyl-D-aspartate (NMDA) receptor
7070707044 7070707044 702675-74-9 N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide (BX-795).
Potent PDK1 inhibitor.
7070707060 7070707060 702674-56-4 N-[3-[[5-Bromo-4-[[2-(1H-imidazol-4-yl)ethyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide (BX-912)
Potent PDK1 inhibitor.
7070707045 7070707045 702676-93-5 N1-[3-[[5-Bromo-2-[[3-[(1-pyrrolidinylcarbonyl)amino]phenyl]amino]-4-pyrimidinyl]amino]propyl]-2,2-dimethylpropanediamide (BX-320)
Potent PDK1 inhibitor.
7070707069 7070707069 40045-50-9 5-[(5-Nitro-2-thiazolyl)thio]-1,3,4-thiadiazol-2-amine (SU 3327).
Selective inhibitor of c-Jun N-terminal kinase (JNK) (IC50 = 0.7 µM). Inhibits the protein-protein interaction between JNK and JIP (IC50 = 239 nM). Displays selectivity over p38 MAPK and Akt. Restores insulin sensitivity in a mouse model of type-2 diabetes
7215270035 7215270035 380315-80-0 N-[[[4-(Acetylamino)phenyl]amino]thioxomethyl]-4-(1,1-dimethylethyl)-benzamide (Tenovin 1).
p53 activator that protects against MDM2-mediated p53 degradation. Elevates levels of p53 and p21CIP/WAF1 and induces expression from an endogenous p53-dependent promoter. Exhibits potent antiproliferative activity in vitro.
7070707137 7070707137 118458-54-1 12,13-Dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione (Arcyriaflavin A).
Inhibitor of cdk4/cyclin D1 (IC50 = 59 nM). Active against CaM kinase II (IC50 = 25 nM) but displays selectivity over several other kinases in vitro (IC50 values for inhibition of PKA and PKC are > 2 and > 100 µM respectively). Inhibits human cytomegalovirus (HCMV) replication in vitro (IC50 = 200 nM).

 

Learn more about other Focused Libraries available from Otava:

 

 

 

 

The libraries (DB, SD, XLS, PDF format) as well as price-list are available on request. Feel free to contact us or use on-line form below to send an inquiry if you are interested to obtain these libraries or if you need more information.

 

 

 

 

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