| Identification | Back Directory | [Name]
CVT-6883 | [CAS]
752222-83-6 | [Synonyms]
GS-6201
CVT-6883
GS6201 CVT6883
GS 6201; GS6201; GS6201; CVT6883; CVT-6883
3-Ethyl-1-propyl-8-(1-(3-(trifluoromethyl)benzyl)-1H-pyrazol-4-yl)-1H-purine-2,6(3H,8H)-dione
3-Ethyl-1-propyl-8-[1-(3-trifluoromethyl-benzyl)-1H-pyrazol-4-yl]-3,7-dihydro-purine-2,6-dione
3-Ethyl-3,9-dihydro-1-propyl-8-[1-[[3-(trifluoroMethyl)phenyl]Methyl]-1H-pyrazol-4-yl]-1H-purine-2,6-dione
1H-Purine-2,6-dione, 3-ethyl-3,9-dihydro-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-4-yl]- | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C21H21F3N6O2 | [MDL Number]
MFCD11042420 | [MOL File]
752222-83-6.mol | [Molecular Weight]
446.43 |
| Chemical Properties | Back Directory | [Boiling point ]
639.6±65.0 °C(Predicted) | [density ]
1.44 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A solid | [pka]
7.69±0.70(Predicted) | [color ]
White to light brown |
| Hazard Information | Back Directory | [Uses]
3-Ethyl-3,9-dihydro-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-4-yl]-1H-purine-2,6-dione, is a novel selective, high-affinity A2B adenosine receptor (AR) antagonist, used for the treatment of inflammatory and angiogenic diseases. | [Biological Activity]
GS-6201 (CVT-6883) is a potent and selective A2B adenosine receptor (A2BAdoR) antagonist. GS-6201 reduces caspase-1 activity in the heart and leads to a more favorable cardiac remodeling in a mouse model of non-reperfused myocardial infarction. Also GS-6201 attenuated vascular remodeling and hypertension in mouse model. | [in vivo]
GS-6201 (CVT-6883) (4 mg/kg; i.p.; every 12 h for 14 days) significantly reduces IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels[2].
GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) leads to a significant attenuation of left and right ventricular enlargement and dysfunction at 7 days, which was maintained at 14 days and also at 28 days[2].
GS-6201 (2 mg/kg; p.o.) treatment shows the Cmax, dAUC and t1/2 are 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively[1]. | Animal Model: | Adult out-bred male CD1 mice (8-12 weeks of age, AMI model)[2] | | Dosage: | 4 mg/kg | | Administration: | i.p.; every 12 h for 14 days | | Result: | Significantly reduced IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels. |
| Animal Model: | Sprague-Dawley rats[1] | | Dosage: | 2 mg/kg | | Administration: | p.o. (Pharmacokinetic Analysis) | | Result: | The Cmax, dAUC and t1/2 were 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively. |
| [storage]
Store at -20°C |
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