| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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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].
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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)). |
| 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, potent and orally available A2B-adenosine receptor antagonist which CV Therapeutics is investigating for the potential treatment of asthma and other conditions related to inflammation and fibrosis.
Drug Indication Investigated for use/treatment in asthma. |
| 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 |
Typically exists as solid at room temperature
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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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