PyrTac-5f
IC50 microM EeACHE 0.060 +/- 0.006 ; HuACHE 0.78 +/- 0.08 ; HuBCHE 12 +/- 1. Activating phosphatase 2A (PP2A) PyrTac-5f at 2.5mg/kg 20min before photothrombosis, and twice per day for 2 days, diminished the infarct volume by 59% compared with controls
General
Type : Derivative of Tacrine, Multitarget, Protein Phosphatase activator, Pyridine
Chemical_Nomenclature : ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate
Canonical SMILES : CCOC(=O)C1=C(N=C2C(=C1)C(=C3CCCCC3=N2)N)C
InChI : InChI=1S\/C16H19N3O2\/c1-3-21-16(20)11-8-12-14(17)10-6-4-5-7-13(10)19-15(12)18-9(11)2\/h8H,3-7H2,1-2H3,(H2,17,18,19)
InChIKey : XGQUEKANWWMGAJ-UHFFFAOYSA-N
Other name(s) : CR80-ITH12246 || ITH12246 || CHEMBL1087194 || BDBM50317074 || Ethyl 5-Amino-2-methyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate
MW : 285.34
Formula : C16H19N3O2
CAS_number :
PubChem : 46861819
UniChem : XGQUEKANWWMGAJ-UHFFFAOYSA-N
Target
Families : PyrTac-5f ligand of proteins in family
ACHE
Protein :
human-ACHE
References (4)
| Title : Tacrines for Alzheimer's disease therapy. III. The PyridoTacrines - de Los Rios_2019_Eur.J.Med.Chem_166_381 |
| Author(s) : de los Rios C , Marco-Contelles J |
| Ref : Eur Journal of Medicinal Chemistry , 166 :381 , 2019 |
| Abstract : |
| PubMedSearch : de Los Rios_2019_Eur.J.Med.Chem_166_381 |
| PubMedID: 30739821 |
| Title : PP2A ligand ITH12246 protects against memory impairment and focal cerebral ischemia in mice - Lorrio_2013_ACS.Chem.Neurosci_4_1267 |
| Author(s) : Lorrio S , Romero A , Gonzalez-Lafuente L , Lajarin-Cuesta R , Martinez-Sanz FJ , Estrada M , Samadi A , Marco-Contelles J , Rodriguez-Franco MI , Villarroya M , Lopez MG , de los Rios C |
| Ref : ACS Chem Neurosci , 4 :1267 , 2013 |
| Abstract : |
| PubMedSearch : Lorrio_2013_ACS.Chem.Neurosci_4_1267 |
| PubMedID: 23763493 |
| Title : Molecular modelling, synthesis and acetylcholinesterase inhibition of ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate - Soriano_2010_Bioorg.Med.Chem.Lett_20_2950 |
| Author(s) : Soriano E , Samadi A , Chioua M , de los Rios C , Marco-Contelles J |
| Ref : Bioorganic & Medicinal Chemistry Lett , 20 :2950 , 2010 |
| Abstract : |
| PubMedSearch : Soriano_2010_Bioorg.Med.Chem.Lett_20_2950 |
| PubMedID: 20350807 |
| Title : Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives - de Los Rios_2010_J.Med.Chem_53_5129 |
| Author(s) : de los Rios C , Egea J , Marco-Contelles J , Leon R , Samadi A , Iriepa I , Moraleda I , Galvez E , Garcia AG , Lopez MG , Villarroya M , Romero A |
| Ref : Journal of Medicinal Chemistry , 53 :5129 , 2010 |
| Abstract : |
| PubMedSearch : de Los Rios_2010_J.Med.Chem_53_5129 |
| PubMedID: 20575555 |