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GS-6201 (CVT-6883) is a selective antagonist of the adenosine A2B receptor, demonstrating high affinity and selectivity with a Ki of 22 nM for human adenosine A2B receptors.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $30 | In Stock | In Stock | |
| 5 mg | $68 | In Stock | In Stock | |
| 10 mg | $123 | In Stock | In Stock | |
| 25 mg | $262 | In Stock | In Stock | |
| 50 mg | $423 | In Stock | In Stock | |
| 100 mg | $636 | - | In Stock | |
| 200 mg | $895 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $75 | In Stock | In Stock |
| Description | GS-6201 (CVT-6883) is a selective antagonist of the adenosine A2B receptor, demonstrating high affinity and selectivity with a Ki of 22 nM for human adenosine A2B receptors. |
| Targets&IC50 | A3:1070 nM(Ki, human), A1:1940 nM(Ki, human), A2B:22 nM(Ki, human), A2A:3280 nM(Ki, human) |
| In vivo | GS-6201 (2 mg/kg; p.o.) treatment displays the Cmax, dAUC and t1/2 are 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively [1]. GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) obviously decreases IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels. GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) causes an obvious attenuation of left and right ventricular enlargement and dysfunction at 7 days, which was maintained at 14 days and also at 28 days [2]. |
| Synonyms | CVT-6883 |
| Molecular Weight | 446.43 |
| Formula | C21H21F3N6O2 |
| Cas No. | 752222-83-6 |
| Smiles | CCCn1c(=O)n(CC)c2[nH]c(nc2c1=O)-c1cnn(Cc2cccc(c2)C(F)(F)F)c1 |
| Relative Density. | 1.44 g/cm3 |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 30 mg/mL (67.2 mM), Sonication and heating to 60℃ are recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 2 mg/mL (4.48 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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