Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C18H20N2O3 |
| Molecular Weight | 312.363 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C(CN(C)C(=O)\C=C\C2=CN=CC=C2)C=C1OC
InChI
InChIKey=HOIFFGYKGILBPW-VQHVLOKHSA-N
InChI=1S/C18H20N2O3/c1-20(18(21)9-7-14-5-4-10-19-12-14)13-15-6-8-16(22-2)17(11-15)23-3/h4-12H,13H2,1-3H3/b9-7+
| Molecular Formula | C18H20N2O3 |
| Molecular Weight | 312.363 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Optical Activity | NONE |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Tue Apr 01 16:29:57 GMT 2025
by
admin
on
Tue Apr 01 16:29:57 GMT 2025
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| Record UNII |
43KJV42JGA
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| Record Status |
Validated (UNII)
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| Record Version |
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Preferred Name | English | ||
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Systematic Name | English |
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785046-87-9
Created by
admin on Tue Apr 01 16:29:57 GMT 2025 , Edited by admin on Tue Apr 01 16:29:57 GMT 2025
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43KJV42JGA
Created by
admin on Tue Apr 01 16:29:57 GMT 2025 , Edited by admin on Tue Apr 01 16:29:57 GMT 2025
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20701430
Created by
admin on Tue Apr 01 16:29:57 GMT 2025 , Edited by admin on Tue Apr 01 16:29:57 GMT 2025
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PRIMARY |
| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Class: Anti-inflammatory; Mechanism of Action: Transforming growth factor beta1 inhibitor, Tumour necrosis factor inhibitor; Highest Development Phase: Discontinued for Glomerulonephritis;
Most Recent Event: 20 Mar 2005 Discontinued - Phase-II for Glomerulonephritis in Japan (PO), 20 Oct 2004 Phase-II clinical trials in Glomerulonephritis in Japan (PO), 20 Feb 2004 Phase-I clinical trials in Glomerulonephritis in Japan (PO)
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ACTIVE MOIETY |
RESULTS: Treatment with TJN-598 prevented an increase in the mesangial area/total glomerular area, in the number of cells in the glomerular cross section and matrix index. TJN-598 also inhibited the increases in the expression of .ALPHA.-smooth muscle actin, the TGF-.BETA.1-positive area, in the number of ED-1 positive cells and proliferating cell nuclear antigen-positive cells in the glomeruli. Furthermore, administration of TJN-598 inhibited increases in the levels of TGF-.BETA.1 protein derived from glomeruli with anti-Thy-1 nephritis. The addition of both TJN-598 and rolipram to the culture supernatant inhibited both increased expression of TGF-.BETA.1 and increases in levels of TNF-.ALPHA. in glomeruli isolated from rats with anti-Thy1 nephritis in a dose-dependent manner.
CONCLUSION: These results suggest that TJN-598, a PDEIV inhibitor, is effective against expansion of mesangial cells, via the suppression of secretion of TGF-.BETA.1 and TNF-.ALPHA. from inflamed glomeruli.
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