GS-6201

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GS-6201 是腺苷 A2B 受体的选择性拮抗剂。 GS-6201 对人腺苷 A2B 受体表现出高亲和力和选择性，Ki 为 22 nM。

GS-6201 is a selective antagonist of adenosine A2B receptor. GS-6201 shows high affinity and selectivity for the human adenosine A2B receptors with a Ki of 22 nM.(In Vivo):In adult out-bred male CD1 mice, GS-6201 (4 mg/kg; i.p.) 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 (4 mg/kg; i.p.) significantly reduces IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels. GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse.

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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 ratsDosage: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.

CVT-6883

Apoptosis

Adenosine Receptor

Antifolate| Drug Metabolite

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752222-83-6

446.434

C21H21F3N6O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (224.00 mM)

CCCn1c(=O)n(CC)c2=NC(N=c2c1=O)c1cnn(Cc2cccc(c2)C(F)(F)F)c1

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(-20℃)

With Ice Pack

≥ 2 years