Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C28H30F2N6O8S |
Molecular Weight | 648.635 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 10 / 10 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@]1(O[C@H](CO)[C@H](O)[C@@H]([C@H]1O)N2C=C(N=N2)C3=CC=CC(F)=C3)S[C@]4([H])O[C@H](CO)[C@H](O)[C@@H]([C@H]4O)N5C=C(N=N5)C6=CC=CC(F)=C6
InChI
InChIKey=YGIDGBAHDZEYMT-MQFIMZJJSA-N
InChI=1S/C28H30F2N6O8S/c29-15-5-1-3-13(7-15)17-9-35(33-31-17)21-23(39)19(11-37)43-27(25(21)41)45-28-26(42)22(24(40)20(12-38)44-28)36-10-18(32-34-36)14-4-2-6-16(30)8-14/h1-10,19-28,37-42H,11-12H2/t19-,20-,21+,22+,23+,24+,25-,26-,27+,28+/m1/s1
Molecular Formula | C28H30F2N6O8S |
Molecular Weight | 648.635 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 10 / 10 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
TD139 is a highly potent, specific inhibitor of the galactoside binding pocket of galectin-3. TD139 is formulated for inhalation, which enables direct targeting the fibrotic tissue in the lungs, while minimizing systemic exposure. TD139 was initially developed by a team of scientists from Lund University, Sweden, and Edinburgh University, the UK. TD-139 is in phase I/II clinical trials for the treatment of idiopathic pulmonary fibrosis.
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Galectin-3 endocytosis by carbohydrate independent and dependent pathways in different macrophage like cell types. | 2012 Jul |
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Galectin-3 deficiency prevents concanavalin A-induced hepatitis in mice. | 2012 Jun |
|
Regulation of transforming growth factor-β1-driven lung fibrosis by galectin-3. | 2012 Mar 1 |
Patents
Sample Use Guides
TD139 is delivered to the lungs of IPF patients using the Plastiape inhaler device at the following 3 doses: 0.3mg, 3mg, and 10mg.
Route of Administration:
Respiratory
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22095546
Primary alveolar epithelial cells from wild-type (WT) mice were plated and treated with transforming growth factor (TGF)-b1 in the presence or absence of 10 uM TD-139. TD-139 (10 uM) blocked TGF-b1–induced
b-catenin phosphorylation as judged by Western blot analysis.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:30:07 UTC 2023
by
admin
on
Sat Dec 16 08:30:07 UTC 2023
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Record UNII |
60Y0GUO72B
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Record Status |
Validated (UNII)
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Record Version |
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FDA ORPHAN DRUG |
757320
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
Related Record | Type | Details | ||
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ACTIVE MOIETY |