产品
编 号：F449051
分子式：C21H21F3N6O2
分子量：446.43
分子式：C21H21F3N6O2
分子量：446.43
产品类型
规格
价格
是否有货
5mg
952
In-stock
10mg
1520
In-stock
25mg
3200
In-stock
50mg
5040
In-stock
结构图
CAS No: 752222-83-6
产品详情
生物活性：
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice.
体内研究：
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.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.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.Animal Model:Adult out-bred male CD1 mice (8-12 weeks of age, AMI model)
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
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.
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice.
体内研究：
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.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.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.Animal Model:Adult out-bred male CD1 mice (8-12 weeks of age, AMI model)
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
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.
产品资料
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