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Details

Stereochemistry ACHIRAL
Molecular Formula C21H19N5O2
Molecular Weight 373.4079
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SEPIMOSTAT

SMILES

NC(=N)C1=CC=C2C=C(OC(=O)C3=CC=C(NC4=NCCN4)C=C3)C=CC2=C1

InChI

InChIKey=QMRJOIUGPCVZPH-UHFFFAOYSA-N
InChI=1S/C21H19N5O2/c22-19(23)16-2-1-15-12-18(8-5-14(15)11-16)28-20(27)13-3-6-17(7-4-13)26-21-24-9-10-25-21/h1-8,11-12H,9-10H2,(H3,22,23)(H2,24,25,26)

HIDE SMILES / InChI

Molecular Formula C21H19N5O2
Molecular Weight 373.4079
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Sepimostat (also known as FUT-187) was developed as a serine protease inhibitor including Clr, Cls, kallikrein, trypsin, plasmin, and thrombin. Sepimostat participated in early phase II clinical study on patients with reflux esophagitis. As a result, sepimostat could be used for postgastrectomy reflux esophagitis at the dose level of 300 mg/day or less. Experiments on rodents have shown that the drug could be also useful in the therapy of alcohol-induced pancreatitis. However, all these studies were discontinued.

Approval Year

PubMed

PubMed

TitleDatePubMed
Pharmacological studies on 6-amidino-2-naphthyl[4-(4,5-dihydro-1H-imidazol-2-yl)amino] benzoate dimethane sulfonate (FUT-187). I: Inhibitory activities on various kinds of enzymes in vitro and anticomplement activity in vivo.
1990 Jan
[Early phase II study of FUT-187 (sepimostat mesilate) on reflux esophagitis--mainly on postgastrectomy reflux esophagitis].
1994 May

Sample Use Guides

FUT-187 (SEPIMOSTAT) was administered orally at the dose of 300 mg/day or 400 mg/day four times daily, after meals and at bedtime, for 4 consecutive weeks
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:28:20 UTC 2023
Edited
by admin
on Fri Dec 15 16:28:20 UTC 2023
Record UNII
5ZFR16F4QQ
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SEPIMOSTAT
INN   MI  
INN  
Official Name English
SEPIMOSTAT [MI]
Common Name English
sepimostat [INN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C783
Created by admin on Fri Dec 15 16:28:20 UTC 2023 , Edited by admin on Fri Dec 15 16:28:20 UTC 2023
Code System Code Type Description
PUBCHEM
108041
Created by admin on Fri Dec 15 16:28:20 UTC 2023 , Edited by admin on Fri Dec 15 16:28:20 UTC 2023
PRIMARY
INN
7003
Created by admin on Fri Dec 15 16:28:20 UTC 2023 , Edited by admin on Fri Dec 15 16:28:20 UTC 2023
PRIMARY
EVMPD
SUB10485MIG
Created by admin on Fri Dec 15 16:28:20 UTC 2023 , Edited by admin on Fri Dec 15 16:28:20 UTC 2023
PRIMARY
CAS
103926-64-3
Created by admin on Fri Dec 15 16:28:20 UTC 2023 , Edited by admin on Fri Dec 15 16:28:20 UTC 2023
PRIMARY
ChEMBL
CHEMBL114586
Created by admin on Fri Dec 15 16:28:20 UTC 2023 , Edited by admin on Fri Dec 15 16:28:20 UTC 2023
PRIMARY
NCI_THESAURUS
C72845
Created by admin on Fri Dec 15 16:28:20 UTC 2023 , Edited by admin on Fri Dec 15 16:28:20 UTC 2023
PRIMARY
EPA CompTox
DTXSID50146144
Created by admin on Fri Dec 15 16:28:20 UTC 2023 , Edited by admin on Fri Dec 15 16:28:20 UTC 2023
PRIMARY
FDA UNII
5ZFR16F4QQ
Created by admin on Fri Dec 15 16:28:20 UTC 2023 , Edited by admin on Fri Dec 15 16:28:20 UTC 2023
PRIMARY
SMS_ID
100000084113
Created by admin on Fri Dec 15 16:28:20 UTC 2023 , Edited by admin on Fri Dec 15 16:28:20 UTC 2023
PRIMARY
MERCK INDEX
m925
Created by admin on Fri Dec 15 16:28:20 UTC 2023 , Edited by admin on Fri Dec 15 16:28:20 UTC 2023
PRIMARY Merck Index
Related Record Type Details
SALT/SOLVATE -> PARENT
SALT/SOLVATE -> PARENT
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ACTIVE MOIETY