T-817 MALEATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H21NO2S.C4H4O4
Molecular Weight	407.481
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)\C=C/C(O)=O.OC1CN(CCCOCCC2=CC=C3SC=CC3=C2)C1

InChI

InChIKey=RLUCYBFCLXANSO-BTJKTKAUSA-N

InChI=1S/C16H21NO2S.C4H4O4/c18-15-11-17(12-15)6-1-7-19-8-4-13-2-3-16-14(10-13)5-9-20-16;5-3(6)1-2-4(7)8/h2-3,5,9-10,15,18H,1,4,6-8,11-12H2;1-2H,(H,5,6)(H,7,8)/b;2-1-

HIDE SMILES / InChI

Molecular Formula	C4H4O4
Molecular Weight	116.0722
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Molecular Formula	C16H21NO2S
Molecular Weight	291.408
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21629767 | https://www.ncbi.nlm.nih.gov/pubmed/21880300 | https://www.ncbi.nlm.nih.gov/pubmed/18573265

T-817 is a thiophenylalkyl derivative patented by Toyama Chemical Co., Ltd. as a neuroprotectant for the treatment of Alzheimer's disease. T-817MA protects neurons against amyloid-b peptide- and hydrogen peroxide-induced neurotoxicity and promoted neurite outgrowth in hippocampal slice cultures and neuronal reaggregation culture. T-817MA protected against nitric oxide-induced neurotoxicity in cultured primary neurons. In a preclinical model of Alzheimer's disease, T-817 increases decreased dopamine levels and tyrosine hydroxylase immunostaining in mice's substantia nigra (SNc) and striatum. Systemic administration of T-817 rescues tau-induced synaptic abnormalities.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Dihydropyrimidinase-related protein 2 4 Target ID: O08553 Gene ID: 12934.0 Gene Symbol: Dpysl2 Target Organism: Mus musculus (Mouse) Sources: https://www.ncbi.nlm.nih.gov/pubmed/29622647	Interacts 323

PubMed

Title	Date	PubMed
A neuroprotective agent, T-817MA (1-{3-[2-(1-benzothiophen-5-yl)ethoxy]propyl} azetidin-3-ol maleate), prevents 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced neurotoxicity in mice.	2008 Oct	18573265
Blocking Effects of Human Tau on Squid Giant Synapse Transmission and Its Prevention by T-817 MA.	2011	21629767
CRMP2-binding compound, edonerpic maleate, accelerates motor function recovery from brain damage.	2018 Apr 6	29622647

Patents

Sample Use Guides

In Vivo Use Guide

mice 30mg/kg

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Sat Dec 16 09:16:51 GMT 2023` Edited by `admin` on `Sat Dec 16 09:16:51 GMT 2023`
Record UNII	0LB9F7I5P3
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

T-817 MALEATE

Common Name

English

T-817MA

Code

English

J2.179.155E

Code

English

3-AZETIDINOL, 1-(3-(2-BENZO(B)THIEN-5-YLETHOXY)PROPYL)-, (2Z)-2-BUTENEDIOATE (1:1)

Systematic Name

English

1-(3-(2-(BENZO(B)THIOPHENE-5-YL)ETHOXY)PROPYL)AZETIDINE-3-OL MALEATE

Systematic Name

English

Code System Code Type Description

SMS_ID

300000036826