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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $37 | In Stock | |
5 mg | $96 | In Stock | |
10 mg | $155 | In Stock | |
25 mg | $328 | In Stock | |
50 mg | $522 | In Stock | |
100 mg | $759 | In Stock | |
1 mL x 10 mM (in DMSO) | $117 | 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 | A2B:22 nM(Ki, human), A2A:3280 nM(Ki, human), A1:1940 nM(Ki, human), A3:1070 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]. |
Alias | CVT-6883 |
Molecular Weight | 446.43 |
Formula | C21H21F3N6O2 |
Cas No. | 752222-83-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/ml (67.2 mM), Sonication and heating to 60℃ are recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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