|
Back to products
Browse products
Approved anticancer agents
Anticancer agents in trials
Anticancer agents
in preclinical trials
Anticancer molecular libraries
Other drug agents
Drug intermediates
Bio-reagents and biochemicals
|
MedKoo product information:
CVT-6883
CVT-6883, a selective A2B adenosine antagonist, represents a novel
potential approach to treating cardiopulmonary diseases. A
pre-clinical study showed that CVT-6883 significantly reduced
elevated markers of inflammation, fibrosis and pulmonary injury in
in vivo preclinical models. An initial Phase 1 study of CVT-6883 has
been completed. In this randomized, double-blind,
placebo-controlled, single ascending dose study in 24 healthy
volunteers, CVT-6883 was well tolerated with no serious adverse
events reported. In 2007, we completed a second Phase 1 trial, an
ascending, multi-dose study in 30 healthy volunteers.
Current developer:
CV Therapeutics
|
MedKoo Code#:
200842
|
|
Name:
CVT-6883
|
|
CAS#:
752222-83-6
Synonym:
Code name: CVT-6883. Chemical name:
3-ethyl-1-propyl-8-(1-(3-trifluoromethylbenzyl)-1H-pyrazol-4-yl)-3,7-dihydropurine-2,6-dione.
IUPAC/Chemical name:
3-ethyl-1-propyl-8-(1-(3-(trifluoromethyl)benzyl)-1H-pyrazol-4-yl)-1H-purine-2,6(3H,7H)-dione
|
|
Chemical structure
|
Theoretical analysis
|
|

|
MedKoo Code#: 200842
Name: CVT-6883
CAS#: 752222-83-6
Chemical Formula: C21H21F3N6O2
Exact Mass: 446.16781
Molecular Weight: 446.42
Elemental Analysis: C, 56.50; H, 4.74; F,
12.77; N, 18.83; O, 7.17
|
|
Availability and price:
CVT-6883 (98%) is in stock.
10 mg / $350.00
50 mg / $1,150.00
100 mg $1,750.00
For quotation, question, and order, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
|
|
Information about this agent
|
CVT-6883, a selective A2B adenosine antagonist,
represents a novel potential approach to treating cardiopulmonary
diseases. A pre-clinical study showed that CVT-6883 significantly
reduced elevated markers of inflammation, fibrosis and pulmonary injury
in in vivo preclinical models. An initial Phase 1 study of CVT-6883 has
been completed. In this randomized, double-blind, placebo-controlled,
single ascending dose study in 24 healthy volunteers, CVT-6883 was well
tolerated with no serious adverse events reported. In 2007, we completed
a second Phase 1 trial, an ascending, multi-dose study in 30 healthy
volunteers.
On November 02, 2007, CV Therapeutics, Inc. announced
that data from a randomized, single-blind, placebo-controlled, multiple
ascending dose Phase 1 study of CVT-6883, a potentially first in class
adenosine A2B antagonist, show that a range of doses were safe and well
tolerated in 30 healthy volunteers. Read more:
http://www.drugs.com/clinical_trials/data-completed-phase-1-studies-novel-adenosine-a2b-antagonist-cvt-6883-show-safety-tolerability-2535.html#ixzz0xk6RUaqu.
1: Ortore G, Martinelli A. A2B receptor ligands:
past, present and future trends. Curr Top Med Chem. 2010;10(9):923-40.
Review. PubMed PMID: 20370659.
2: Kalla RV, Zablocki J, Tabrizi MA, Baraldi PG. Recent developments in
A2B adenosine receptor ligands. Handb Exp Pharmacol. 2009;(193):99-122.
Review. PubMed PMID: 19639280.
3: Chen H, Yang D, Carroll SH, Eltzschig HK, Ravid K. Activation of the
macrophage A2b adenosine receptor regulates tumor necrosis factor-alpha
levels following vascular injury. Exp Hematol. 2009 May;37(5):533-8.
PubMed PMID: 19375644.
4: Chen C, Bajpai L, Mollova N, Leung K. Sensitive and cost-effective
LC-MS/MS method for quantitation of CVT-6883 in human urine using sodium
dodecylbenzenesulfonate additive to eliminate adsorptive losses. J
Chromatogr B Analyt Technol Biomed Life Sci. 2009 Apr 1;877(10):943-7.
Epub 2009 Feb 24. PubMed PMID: 19282253.
5: Ham J, Rees DA. The adenosine a2b receptor: its role in inflammation.
Endocr Metab Immune Disord Drug Targets. 2008 Dec;8(4):244-54. Review.
PubMed PMID: 19075778.
6: Kalla RV, Zablocki J. Progress in the discovery of selective, high
affinity A(2B) adenosine receptor antagonists as clinical candidates.
Purinergic Signal. 2009 Mar;5(1):21-9. Epub 2008 Jun 21. PubMed PMID:
18568423; PubMed Central PMCID: PMC2721775.
7: Mustafa SJ, Nadeem A, Fan M, Zhong H, Belardinelli L, Zeng D. 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. J Pharmacol Exp Ther. 2007
Mar;320(3):1246-51. Epub 2006 Dec 11. PubMed PMID: 17159162.
8: Sun CX, Zhong H, Mohsenin A, Morschl E, Chunn JL, Molina JG,
Belardinelli L, Zeng D, Blackburn MR. Role of A2B adenosine receptor
signaling in adenosine-dependent pulmonary inflammation and injury. J
Clin Invest. 2006 Aug;116(8):2173-2182. PubMed PMID: 16841096; PubMed
Central PMCID: PMC1501110.
|
Contact MedKoo:
Email:
sales@medkoo.com
(Keyword; CAS#; MedKoo code#)
|