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
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)
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.
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
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
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8185343
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
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Record UNII |
5ZFR16F4QQ
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Record Status |
Validated (UNII)
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NCI_THESAURUS |
C783
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108041
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m925
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PRIMARY | Merck Index |
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |