| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
CVT-6883 targets the adenosine A2B receptor. It acts as a selective antagonist. It has a Ki of 22 nM for human A2B receptors. It shows >50-fold selectivity over A3, A1, and A2A receptors. By blocking A2B receptors, it modulates inflammation and fibrosis.
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| ln Vitro |
CVT-6883 is a selective A2B receptor antagonist with a Ki of 22 nM. It reduces caspase-1 activity in the heart. It attenuates cardiac remodeling after acute myocardial infarction. It attenuates allergen-induced responses in sensitized mice.
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| ln Vivo |
The plasma levels of IL-6, TNF-α, E-selectin, ICAM-1, and VCAM are dramatically reduced by GS-6201 (CVT-6883) (4 mg/kg; i.p.; every 12 hours for 14 days) [ 2]. Left and right ventricular hypertrophy and dysfunction were brought on by GS-6201 (4 mg/kg; intraperitoneal; every 12 hours for 14 days); these effects were markedly reduced after 7 days and persisted after 14 and 28 days [2]. The oral GS-6201 (2 mg/kg) therapy showed a Cmax of 1110 ng/mL, a dAUC of 6500 ng·h/mL, and a t1/2 of 4.25 hours, respectively [1].
CVT-6883 significantly reduces IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels in mice. It reduces caspase-1 activity in the heart and attenuates cardiac remodeling after acute myocardial infarction. It attenuates NECA-induced responses in sensitized mice. |
| Enzyme Assay |
CVT-6883 is evaluated in cell-free receptor binding assays to determine its affinity for adenosine receptors. Radioligand binding displacement assays are performed using membrane preparations expressing A2B, A1, A2A, and A3 receptors. Ki values are determined to quantify the potency of A2B receptor antagonism.
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| Cell Assay |
CVT-6883 is assessed in cell-based assays using cells expressing adenosine receptors. Cells are treated with CVT-6883, and receptor activity is measured by assessing downstream signaling pathways, such as cAMP accumulation. The compound's ability to antagonize A2B receptor-mediated responses is evaluated.
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| Animal Protocol |
Animal/Disease Models: Adult outbred male CD1 mice (8-12 weeks old, AMI model) [2]
Doses: 4 mg/kg Route of Administration: intraperitoneal (ip) injection; every 12 hrs (hrs (hours)) for 14 days Experimental Results: IL-6 , TNF-α, E-selectin, ICAM-1 and VCAM plasma levels were Dramatically diminished. Animal/Disease Models: SD (SD (Sprague-Dawley)) rat[1] Doses: 2 mg/kg Route of Administration: po (pharmacokinetic/PK/PK analysis) Experimental Results: Cmax, dAUC and t1/2 were 1110 ng/mL, 6500 ng·h/ mL and 4.25 hrs (hrs (hours)). CVT-6883 is administered intraperitoneally in animal models to evaluate its cardioprotective and anti-inflammatory effects. It is dosed at 4 mg/kg every 12 h for 14 days. Efficacy is assessed by measuring inflammatory markers, cardiac function, and remodeling. |
| ADME/Pharmacokinetics |
CVT-6883 has a molecular weight of 460.45 and a molecular formula of C23H21N5O3S. It has a CAS number of 752222-83-6. The compound is soluble in DMSO. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CVT-6883. The compound is for research use only and is not intended for human therapeutic use. It is a selective A2B receptor antagonist.
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| References |
[1]. Elzein E, et al. Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. J Med Chem. 2008 Apr 10;51(7):2267-78.
[2]. Toldo S, et al. GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J Pharmacol Exp Ther. 2012 Dec;343(3):587-95. [3]. Mustafa SJ, et al. 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. |
| Additional Infomation |
CVT-6883 is a selective, orally effective A2B adenosine receptor antagonist. CV Therapeutics is investigating its potential efficacy in treating asthma and other conditions related to inflammation and fibrosis.
Drug Indications It has been studied for the treatment of asthma. CVT-6883 is a selective A2B adenosine receptor antagonist. It is also known as GS-6201. It reduces cardiac remodeling after myocardial infarction. It is not approved for clinical use. |
| Molecular Formula |
C21H21F3N6O2
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|---|---|
| Molecular Weight |
446.42
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| Exact Mass |
446.168
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| CAS # |
752222-83-6
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| PubChem CID |
11270783
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| Appearance |
White to light brown solid powder
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| Density |
1.44
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| Boiling Point |
538.4ºC at 760 mmHg
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| Index of Refraction |
1.64
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| LogP |
3.246
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
708
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCN1C(=O)C2=C(NC(=N2)C3=CN(CC4=CC(=CC=C4)C(F)(F)F)N=C3)N(CC)C1=O
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| InChi Key |
KOYXXLLNCXWUNF-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
3-ethyl-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]-7H-purine-2,6-dione
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| Synonyms |
CVT-6883; CVT 6883; CVT6883
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~224.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (4.48 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (4.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2400 mL | 11.2002 mL | 22.4004 mL | |
| 5 mM | 0.4480 mL | 2.2400 mL | 4.4801 mL | |
| 10 mM | 0.2240 mL | 1.1200 mL | 2.2400 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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