Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H21F3N6O2 |
Molecular Weight | 446.4256 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCN1C(=O)N(CC)C2=C(NC(=N2)C3=CN(CC4=CC=CC(=C4)C(F)(F)F)N=C3)C1=O
InChI
InChIKey=KOYXXLLNCXWUNF-UHFFFAOYSA-N
InChI=1S/C21H21F3N6O2/c1-3-8-30-19(31)16-18(29(4-2)20(30)32)27-17(26-16)14-10-25-28(12-14)11-13-6-5-7-15(9-13)21(22,23)24/h5-7,9-10,12H,3-4,8,11H2,1-2H3,(H,26,27)
Molecular Formula | C21H21F3N6O2 |
Molecular Weight | 446.4256 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/23225885Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/16841096 | https://www.ncbi.nlm.nih.gov/pubmed/18321039
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23225885
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/16841096 | https://www.ncbi.nlm.nih.gov/pubmed/18321039
CVT-6883 (GS 6201) is an A2B adenosine receptor antagonist originated by CV Therapeutics and developed by Gilead Sciences or the treatment of pulmonary diseases. In vitro studies have suggested that the activation of the A2B adenosine receptor may potentially have Proinflammatory and profibrotic effects that could be significant in the development of lung diseases. In adenosine deaminase (ADA) deficient mice, treatment with GS 6201 resulted in significantly less pulmonary inflammation, fibrosis, and alveolar airway enlargement compared with ADA-deficient mice treated with placebo. A range of doses of GS 6201 was well tolerated in healthy volunteers in a phase I multiple ascending dose trial.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL255 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16841096 |
8.3 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Sources: goo.gl/g7d5Zf |
Primary | Unknown Approved UseUnknown |
||
Sources: goo.gl/g7d5Zf |
Primary | Unknown Approved UseUnknown |
||
Sources: goo.gl/g7d5Zf |
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23225885
Experimental autoimmune encephalomyelitis (EAE) were treated via i.p. injection of CVT-6883 (0.3, 1, or 3 mg/kg, dissolved in saline) once daily from day 3 till the end of the study (day 19).
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23225885
Freshly isolated human dendritic cells were incubated in the presence of CVT-6883 (30, 100, or 300 nM) for 30 min before 5’-Nethylcarboxamidoadenosine (NECA). CVT-6883 significantly reduced adenosine-mediated IL-6 production by dendritic cells.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:11:21 GMT 2023
by
admin
on
Sat Dec 16 09:11:21 GMT 2023
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Record UNII |
67CKV7X08G
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Record Status |
Validated (UNII)
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Record Version |
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CHEMBL260933
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ALTERNATIVE |
Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
IC50
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Related Record | Type | Details | ||
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ACTIVE MOIETY |