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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

 

References

 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.

 

 

 

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