Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H15ClN2O4S2 |
| Molecular Weight | 434.916 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)CCCC1=CC2=CC(Cl)=CC=C2N1S(=O)(=O)C3=CC4=C(C=C3)N=CS4
InChI
InChIKey=OQDQIFQRNZIEEJ-UHFFFAOYSA-N
InChI=1S/C19H15ClN2O4S2/c20-13-4-7-17-12(8-13)9-14(2-1-3-19(23)24)22(17)28(25,26)15-5-6-16-18(10-15)27-11-21-16/h4-11H,1-3H2,(H,23,24)
| Molecular Formula | C19H15ClN2O4S2 |
| Molecular Weight | 434.916 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: Q07869 Gene ID: 5465.0 Gene Symbol: PPARA Target Organism: Homo sapiens (Human) |
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Target ID: Q03181|||Q9BUD4 Gene ID: 5467.0 Gene Symbol: PPARD Target Organism: Homo sapiens (Human) |
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Target ID: P37231|||Q15179 Gene ID: 5468.0 Gene Symbol: PPARG Target Organism: Homo sapiens (Human) |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 12:04:13 GMT 2023
by
admin
on
Sat Dec 16 12:04:13 GMT 2023
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| Record UNII |
28Q8AG0PYL
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| Record Status |
Validated (UNII)
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| Record Version |
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Official Name | English | ||
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Code | English |
| Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
470315
Created by
admin on Sat Dec 16 12:04:13 GMT 2023 , Edited by admin on Sat Dec 16 12:04:13 GMT 2023
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EU-Orphan Drug |
EU/3/14/1361
Created by
admin on Sat Dec 16 12:04:13 GMT 2023 , Edited by admin on Sat Dec 16 12:04:13 GMT 2023
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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DB14801
Created by
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PRIMARY | |||
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28Q8AG0PYL
Created by
admin on Sat Dec 16 12:04:13 GMT 2023 , Edited by admin on Sat Dec 16 12:04:13 GMT 2023
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PRIMARY | |||
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SUB184623
Created by
admin on Sat Dec 16 12:04:13 GMT 2023 , Edited by admin on Sat Dec 16 12:04:13 GMT 2023
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PRIMARY | |||
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EU/3/14/1362(POSITIVE)
Created by
admin on Sat Dec 16 12:04:13 GMT 2023 , Edited by admin on Sat Dec 16 12:04:13 GMT 2023
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PRIMARY | On 19 November 2014, orphan designation (EU/3/14/1362) was granted by the European Commission to Inventiva, France, for 1-(6-benzothiazolylsulfonyl)-5-chloro-1H-indole-2-butanoic acid for the treatment of idiopathic pulmonary fibrosis. | ||
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C166556
Created by
admin on Sat Dec 16 12:04:13 GMT 2023 , Edited by admin on Sat Dec 16 12:04:13 GMT 2023
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10474
Created by
admin on Sat Dec 16 12:04:13 GMT 2023 , Edited by admin on Sat Dec 16 12:04:13 GMT 2023
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PRIMARY | |||
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68677842
Created by
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PRIMARY | |||
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927961-18-0
Created by
admin on Sat Dec 16 12:04:13 GMT 2023 , Edited by admin on Sat Dec 16 12:04:13 GMT 2023
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PRIMARY | |||
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100000170566
Created by
admin on Sat Dec 16 12:04:13 GMT 2023 , Edited by admin on Sat Dec 16 12:04:13 GMT 2023
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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TARGET -> AGONIST | |||
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TARGET -> AGONIST |
AGONIST
EC50
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TARGET -> AGONIST |
AGONIST
EC50
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
RESULTS: In mice, IVA337 was associated with decreased extracellular matrix (ECM) deposition and reduced expression of phosphorylated SMAD2/3-intracellular effector of transforming growth factor (TGF)-.BETA.1. Although the antifibrotic effect of pan PPAR was similar to that of PPAR.GAMMA. agonist alone, a significant downregulation of several markers of inflammation was associated with IVA337. Despite its anti-inflammatory and antifibrotic properties, IVA337 did not interfere with wound closure. In vitro effects of IVA337 included attenuation of transcription of ECM genes and alteration of canonical and non-canonical TGF-.BETA. signalling pathways.
CONCLUSIONS: These findings indicate that simultaneous activation of all three PPAR isoforms exerts a dampening effect on inflammation and fibrosis, making IVA337 a potentially effective therapeutic candidate in the treatment of fibrotic diseases including SSc.
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