GS-6201 (CVT-6883) 是一种选择性的腺苷A2B受体拮抗剂。GS-6201 对人腺苷 A2B 受体具有高亲和力和选择性 (Ki=22 nM)。GS-6201 降低了小鼠急性心肌梗死 (AMI) 后心脏中 caspase-1 的活性，并减弱了心脏重塑。GS-6201 减弱了致敏小鼠 NECA，AMP 或变应原诱导的气道反应性。
| 生物活性 | GS-6201 (CVT-6883) is a selectiveadenosine A2B receptorantagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM)[1]. GS-6201 reducescaspase-1activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse[2]. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice[3]. |
| IC50& Target | Ki: 22 nM (human A2B receptors), 1070 nM (human A3 receptors), 1940 nM (human A1 receptors), 3280 nM (human A2A receptors)[1] |
体内研究
(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 t1/2are 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 t1/2were 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 20 mg/mL(44.80 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.2400 mL | 11.2000 mL | 22.3999 mL | | 5 mM | 0.4480 mL | 2.2400 mL | 4.4800 mL | | 10 mM | 0.2240 mL | 1.1200 mL | 2.2400 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2 mg/mL (4.48 mM); Suspended solution; Need ultrasonic
此方案可获得 2 mg/mL (4.48 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2 mg/mL (4.48 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (4.48 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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