Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C25H27NO5 |
| Molecular Weight | 421.4856 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC1=C(CCOC2=CC=C3[C@H](CC(O)=O)CCC3=C2)N=C(O1)C4=CC=C(OC)C=C4
InChI
InChIKey=BINJXYDNGPHRGX-SFHVURJKSA-N
InChI=1S/C25H27NO5/c1-3-23-22(26-25(31-23)16-6-8-19(29-2)9-7-16)12-13-30-20-10-11-21-17(14-20)4-5-18(21)15-24(27)28/h6-11,14,18H,3-5,12-13,15H2,1-2H3,(H,27,28)/t18-/m0/s1
| Molecular Formula | C25H27NO5 |
| Molecular Weight | 421.4856 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 19:47:52 GMT 2023
by
admin
on
Fri Dec 15 19:47:52 GMT 2023
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| Record UNII |
4TW7R18VOJ
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| Record Status |
Validated (UNII)
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| Record Version |
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1257641-15-8
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49793231
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2081127-92-4
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admin on Fri Dec 15 19:47:52 GMT 2023 , Edited by admin on Fri Dec 15 19:47:52 GMT 2023
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4TW7R18VOJ
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CHEMBL3545176
Created by
admin on Fri Dec 15 19:47:52 GMT 2023 , Edited by admin on Fri Dec 15 19:47:52 GMT 2023
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ACTIVE MOIETY |
T3D-959 significantly improved spatial learning and memory in i.c STZ-treated rats. Mechanistically, T3D-959 significantly improved culture viability and brain morphology, reduced levels of oxidative stress and A.BETA., and normalized expression of phospho-tau, choline acetyltransferase, and myelin-associated glycoprotein. Protective effects occurred even at the lowest tested dose of T3D-959. Pre-clinical proof of concept has been demonstrated that T3D-959 can improve multiple pathologies of AD resulting in significant improvements in cognitive function and molecular and biochemical indices of neurodegeneration. These results support the theses that (1) effective disease modification in AD can be achieved by targeting relevant nuclear receptors, and (2) treating AD as a metabolic disease has the potential to be disease remedial. A Phase 2a trial of T3D-959 in mild-to-moderate AD patients has been initiated (ClinicalTrials.gov identifier NCT02560753).
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ACTIVE MOIETY |
T3D-959 is a small molecule dual nuclear receptor agonist being tested as a potential treatment for Alzheimer's disease. It has been shown to have insulin-sensitizing activity in rats, with the ability to improve multiple pathologies of Alzheimer's disease. It is safe and well tolerated in humans. The drug helps correct insulin resistance in the brain, which is highly correlated with Alzheimer's disease and may be a key driver of Alzheimer's pathology.
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ACTIVE MOIETY |
Originator: Bayer HealthCare Pharmaceuticals; Developer: DARA BioSciences, T3D Therapeutics; Class: Antihyperglycaemic, Insulin sensitiser, Small molecule; Mechanism of Action: Peroxisome proliferator-activated receptor delta agonist, Peroxisome proliferator-activated receptor gamma agonist; Highest Development Phases: Phase I/II Alzheimer's disease, Discontinued for Dyslipidaemia, Type 2 diabetes mellitus; Most Recent Events: 01 Jul 2015 Phase-I/II clinical trials in Alzheimer's disease (In the elderly, In adults) in USA (PO) (NCT02560753), 18 Jun 2013 Discontinued - Phase-I for Type-2 diabetes mellitus in USA (PO), 18 Jun 2013 Discontinued - Phase-I for Dyslipidaemias in USA (PO)
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