Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C57H86N2O14 |
| Molecular Weight | 1023.2977 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 17 / 17 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@@H](C)[C@@](O)(O1)C(=O)C(=O)N3CCCC[C@@]3([H])C(=O)O[C@@]([H])(CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)[C@]4([H])CC[C@@]([H])(ON4C5=CC=CC=C5)\C=C(C)\[C@H](C2)OC)[C@H](C)C[C@@H]6CC[C@@H](O)[C@@H](C6)OC
InChI
InChIKey=WZFNBQBUDJACCD-ZSYWEHCUSA-N
InChI=1S/C57H86N2O14/c1-33-26-37(5)51(62)53(70-10)52(63)38(6)27-34(2)47(61)32-49(35(3)28-40-20-24-46(60)50(30-40)69-9)71-56(66)45-18-14-15-25-58(45)55(65)54(64)57(67)39(7)19-21-42(72-57)31-48(68-8)36(4)29-43-22-23-44(33)59(73-43)41-16-12-11-13-17-41/h11-13,16-17,27,29,33-35,37,39-40,42-46,48-50,52-53,60,63,67H,14-15,18-26,28,30-32H2,1-10H3/b36-29+,38-27+/t33-,34+,35+,37+,39+,40-,42-,43+,44-,45-,46+,48-,49-,50+,52+,53-,57+/m0/s1
| Molecular Formula | C57H86N2O14 |
| Molecular Weight | 1023.2977 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 17 / 17 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
ILS 920 (previously known as WAY-265920) was developed for the treatment of stroke. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS 920 successfully completed phase I clinical trial where was determine the safety, tolerability, pharmacokinetics, and pharmacodynamics after administration of ascending single intravenous (IV) doses to healthy adult subjects. However, information about the further development of this drug is not available.
Originator
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:38:20 GMT 2023
by
admin
on
Sat Dec 16 11:38:20 GMT 2023
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| Record UNII |
F2D5P81X82
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| Record Status |
Validated (UNII)
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DB15422
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F2D5P81X82
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892494-07-4
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300000041430
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ACTIVE MOIETY |
Originator: Wyeth; Developer: Pfizer; Class: Neuroprotectant; Mechanism of Action: Immunophilin inhibitor; Highest Development Phase: Discontinued for Stroke; Most Recent Event: 15 Oct 2009 Wyeth has been acquired by Pfizer.
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ACTIVE MOIETY |
Immunophilin ligands, such as rapamycin, have potent neurotrophic activities in vitro, and have been implicated as potential treatments for stroke and Parkinson's disease. A brain-penetrant, nonimmuno-suppressive rapalog, ILS-920, has demonstrated a higher binding affinity to FKBP52 versus FKBP12. In a rat permanent middle cerebral artery occlusion (MCAO) model of stroke, ILS-920 reduces neurological deficits even when administered up to 24 hours post stroke, and this improvement in functional recovery is sustained for at least 90 days. Immuno-histochemical and cell culture analyses showed that ILS-920 protects neurons, oligodendrocytes, and astrocytes, reduces postischemic inflammatory responses and promotes expression of regenerative and oligodendrocyte maturation markers.
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