Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C24H23F3N2O5 |
Molecular Weight | 476.445 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NOC(=O)C2=CC=C(NC(=O)C(O)(CC(C)(C)C3=C4OCCC4=CC=C3)C(F)(F)F)C=C12
InChI
InChIKey=VRZVKIJRJRBQJT-HSZRJFAPSA-N
InChI=1S/C24H23F3N2O5/c1-13-17-11-15(7-8-16(17)20(30)34-29-13)28-21(31)23(32,24(25,26)27)12-22(2,3)18-6-4-5-14-9-10-33-19(14)18/h4-8,11,32H,9-10,12H2,1-3H3,(H,28,31)/t23-/m1/s1
Molecular Formula | C24H23F3N2O5 |
Molecular Weight | 476.445 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/14694204Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/22235147
Sources: https://www.ncbi.nlm.nih.gov/pubmed/14694204
Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/22235147
(+)-ZK 216348 is a selective nonsteroidal glucocorticoid receptor (GR) agonist. (+)-ZK 216348 shows anti-inflammatory activity comparable to prednisolone for both systemic and topical application. (+)-ZK 216348 showed no negative effects on intestinal epithelial migration or proliferation. This compound is a promising candidate for the treatment of acute inflammatory conditions. It was tested as a drug for the inflammatory bowel disease management.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2034 |
20.3 nM [IC50] | ||
Target ID: CHEMBL208 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14694204 |
20.4 nM [IC50] | ||
Target ID: CHEMBL1994 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14694204 |
79.9 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects. | 2004 Jan 6 |
|
Effects of dissociated glucocorticoids on OPG and RANKL in osteoblastic cells. | 2006 May |
|
Molecular mechanisms of glucocorticoid action and selective glucocorticoid receptor agonists. | 2007 Sep 15 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22235147
1 or 10 mg/kg BW
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22295067
The treatment of IEC-6 cells treated with ZK216348 at concentrations of 1–20 uM showed no effect on cell apoptosis.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:26:16 GMT 2023
by
admin
on
Sat Dec 16 11:26:16 GMT 2023
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Record UNII |
8BY7XK862L
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Record Status |
Validated (UNII)
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Record Version |
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Code | English | ||
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669073-68-1
Created by
admin on Sat Dec 16 11:26:16 GMT 2023 , Edited by admin on Sat Dec 16 11:26:16 GMT 2023
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NON-SPECIFIC STEREOCHEMISTRY | |||
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92293311
Created by
admin on Sat Dec 16 11:26:16 GMT 2023 , Edited by admin on Sat Dec 16 11:26:16 GMT 2023
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PRIMARY | |||
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8BY7XK862L
Created by
admin on Sat Dec 16 11:26:16 GMT 2023 , Edited by admin on Sat Dec 16 11:26:16 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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ACTIVE MOIETY |