MGS0274

General

Type : Not A\/B H target, Pro-Drug, Drug

Chemical_Nomenclature : (1S,2S,3S,5R,6S)-2-Amino-3-fluoro-6-(((S)-1-(((((1R,2S,5R)-2-isopropyl-5-methylcyclohexyl)oxy)carbonyl)oxy)ethoxy)carbonyl)bicyclo[3.1.0]hexane-2-carboxylic acid

Canonical SMILES : CC1CCC(C(C1)OC(=O)OC(C)OC(=O)C2C3C2C(C(C3)F)(C(=O)O)N)C(C)C

InChI : InChI=1S\/C21H32FNO7\/c1-9(2)12-6-5-10(3)7-14(12)30-20(27)29-11(4)28-18(24)16-13-8-15(22)21(23,17(13)16)19(25)26\/h9-17H,5-8,23H2,1-4H3,(H,25,26)\/t10-,11+,12+,13+,14-,15+,16+,17+,21+\/m1\/s1

InChIKey : IPAZEPBIOFZFEF-UZEWAWMVSA-N

Other name(s) : SCHEMBL16610461  ||  HY-131336  ||  CS-0133425  ||  TS-134  ||  MGS0274 besylatee


MW : 429.5

Formula : C21H32FNO7

CAS_number :

PubChem : 72550767

UniChem : IPAZEPBIOFZFEF-UZEWAWMVSA-N

Target

Families : Carb_B_Chordata

References (3)

Title : Bottom-up physiologically based pharmacokinetic modeling for predicting the human pharmacokinetic profiles of the ester prodrug MGS0274 and its active metabolite MGS0008, a metabotropic glutamate 2\/3 receptor agonist - Ochi_2022_Xenobiotica__1
Author(s) : Ochi M , Kinoshita K , Yamaguchi JI , Endo H
Ref : Xenobiotica , :1 , 2022
Abstract :
PubMedSearch : Ochi_2022_Xenobiotica__1
PubMedID: 35296225

Title : Discovery of MGS0274, an ester prodrug of a metabotropic glutamate receptor 2\/3 agonist with improved oral bioavailability - Urabe_2020_Eur.J.Med.Chem_203_112521
Author(s) : Urabe H , Miyakoshi N , Ohtake N , Nozoe A , Ochi M , Fukasawa M , Kinoshita K , Yamaguchi JI , Marumo T , Hikichi H , Chaki S , Hashihayata T
Ref : Eur Journal of Medicinal Chemistry , 203 :112521 , 2020
Abstract :
PubMedSearch : Urabe_2020_Eur.J.Med.Chem_203_112521
PubMedID: 32698110

Title : Safety and pharmacokinetic profiles of MGS0274 besylate (TS-134), a novel metabotropic glutamate 2\/3 receptor agonist prodrug, in healthy subjects - Watanabe_2020_Br.J.Clin.Pharmacol_86_2286
Author(s) : Watanabe M , Marcy B , Kinoshita K , Fukasawa M , Hikichi H , Chaki S , Okuyama S , Gevorkyan H , Yoshida S
Ref : British Journal of Clinical Pharmacology , 86 :2286 , 2020
Abstract :
PubMedSearch : Watanabe_2020_Br.J.Clin.Pharmacol_86_2286
PubMedID: 32353162