Details
Stereochemistry | ACHIRAL |
Molecular Formula | C38H43N3O4S |
Molecular Weight | 637.831 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCOC1=CC=C(C=N1)C2=CC=C(CN3C(CC(C)(C)C(O)=O)=C(SC(C)(C)C)C4=C3C=CC(OCC5=NC=C(C)C=C5)=C4)C=C2
InChI
InChIKey=DFQGDHBGRSTTHX-UHFFFAOYSA-N
InChI=1S/C38H43N3O4S/c1-8-44-34-18-14-28(22-40-34)27-12-10-26(11-13-27)23-41-32-17-16-30(45-24-29-15-9-25(2)21-39-29)19-31(32)35(46-37(3,4)5)33(41)20-38(6,7)36(42)43/h9-19,21-22H,8,20,23-24H2,1-7H3,(H,42,43)
Molecular Formula | C38H43N3O4S |
Molecular Weight | 637.831 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://www.biospace.com/News/amira-pharmaceuticals-inc-announces-am103-and/187186http://adisinsight.springer.com/drugs/800027280Curator's Comment: Description was created based on several sources, including
http://www.generon.co.uk/amine-oxides-1830/gsk2190915-sodium-salt-gsk-2190915a-231013117.html
https://www.ncbi.nlm.nih.gov/pubmed/23331559
Sources: http://www.biospace.com/News/amira-pharmaceuticals-inc-announces-am103-and/187186http://adisinsight.springer.com/drugs/800027280
Curator's Comment: Description was created based on several sources, including
http://www.generon.co.uk/amine-oxides-1830/gsk2190915-sodium-salt-gsk-2190915a-231013117.html
https://www.ncbi.nlm.nih.gov/pubmed/23331559
Fiboflapon sodium (GSK2190915) is a high affinity 5-lipoxygenase-activating protein inhibitor being developed for the treatment of asthma. The compound was originally developed by Amira Pharmaceuticals. Fiboflapon sodium (GSK2190915) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. GSK2190915 also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model. Oral administration of Fiboflapon sodium (GSK2190915) (1 mg/kg) resulted in sustained inhibition of ex vivo ionophore-challenged whole blood LTB4 biosynthesis with >90% inhibition for up to 12 h and an EC50 of approximately 7 nM. When rat lungs were challenged in vivo with calcium-ionophore, Fiboflapon sodium inhibited LTB4 and cysteinyl leukotriene (CysLT) production with ED50s of 0.12 mg/kg and 0.37 mg/kg, respectively. Fiboflapon sodium is in Phase-II for Asthma (Adjunctive treatment) in Poland, Ukraine, Bulgaria, USA, United Kingdom and Canada (PO).
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4550 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22059882 |
2.9 nM [IC50] | ||
Target ID: CHEMBL4550 Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=22059882 |
2.9 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Sample Use Guides
Patients receive 100mg of GSK2190915 (FIBOFLAPON) once daily for up to 16 days followed by a wash out period of at least 14 days before they cross over onto the placebo arm of the study.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=22059882
Curator's Comment: 11cc (FIBOFLAPON) has a potency of 2.9 nM in FLAP binding, an IC(50) of 76 nM for inhibition of LTB(4) in human blood (5 h incubation) and excellent preclinical toxicology and pharmacokinetics in rat and dog. 11cc also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model
Unknown
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 19:39:57 UTC 2023
by
admin
on
Fri Dec 15 19:39:57 UTC 2023
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Record UNII |
Y1NA96IX3T
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Record Status |
Validated (UNII)
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DB06346
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44473151
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CHEMBL1922660
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C169978
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936350-00-4
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Y1NA96IX3T
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
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SALT/SOLVATE -> PARENT |
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