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)
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 |
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Sources: goo.gl/g7d5Zf |
Primary | Unknown Approved UseUnknown |
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Sources: goo.gl/g7d5Zf |
Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Effect of a specific and selective A(2B) adenosine receptor antagonist on adenosine agonist AMP and allergen-induced airway responsiveness and cellular influx in a mouse model of asthma. | 2007 Mar |
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Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. | 2008 Apr 10 |
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Sensitive and cost-effective LC-MS/MS method for quantitation of CVT-6883 in human urine using sodium dodecylbenzenesulfonate additive to eliminate adsorptive losses. | 2009 Apr 1 |
|
Activation of the macrophage A2b adenosine receptor regulates tumor necrosis factor-alpha levels following vascular injury. | 2009 May |
|
Alterations in adenosine metabolism and signaling in patients with chronic obstructive pulmonary disease and idiopathic pulmonary fibrosis. | 2010 Feb 16 |
Patents
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.
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67CKV7X08G
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DB05936
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752222-83-6
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CHEMBL260933
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11270783
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1215343-16-0
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ALTERNATIVE |
ACTIVE MOIETY