Valsarta (CGP 48933) 是血管紧张素 II (angiotensin II) 受体拮抗剂,有潜力用于高血压和心力衰竭的研究。
生物活性 | Valsartan (CGP 48933) is anangiotensin IIreceptor antagonist and has the potential for high blood pressure and heart failure research[1]. |
体外研究 (In Vitro) | Valsartan (CGP 48933) is a synthetic non-peptide angiotensin II type 1 receptor antagonist that dilates blood vessels and reduces blood pressure by blocking the action of angiotensin. Valsartan significantly decreases the expression of AT1R in ageing aorta endothelial cells[1]. The pretreatment of valsartan results in an inhibition of TLR2 signaling and proinflammatory cytokines. The expression of AGTR1 is up-regulated after alcohol exposure, and is blocked by valsartan pretreatment[2].
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体内研究 (In Vivo) | Valsartan (CGP 48933) significantly attenuates the expression of TGF-β/Smad, Hif-1α and fibrosis-related protein in rats after MI. Heart function, infarcted size, wall thickness as well as myocardial vascularization of ischaemic hearts are also significantly improved by valsartan compared with saline and hydralazine[3]. Valsartan partially reverses the effects of high-salt diet on hypertension, cardiac injuries such as fibrosis and inflammatory cell infiltration, and inhibition of aquaporin 1 and angiogenic factors; valsartan alone does not exert such effects[4]. Valsartan is an effective antidepressant/antianxiety reagent and can promote the hippocampal neurogenesis and expression of BDNF. Chronic administration of valsartan (5-40 mg/kg/d, p.o.) increases the time spent in the center of the field in OFT and the latency to eat in NSF, reduces the immobility time in both TST and FST, and increases the sucrose preference in SPT[5].
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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 | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(114.81 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) 配制储备液 1 mM | 2.2961 mL | 11.4805 mL | 22.9611 mL | 5 mM | 0.4592 mL | 2.2961 mL | 4.5922 mL | 10 mM | 0.2296 mL | 1.1481 mL | 2.2961 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 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: 50%PEG300 50% saline Solubility: 10 mg/mL (22.96 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.74 mM); Suspended solution
此方案可获得 ≥ 2.5 mg/mL (5.74 mM,饱和度未知) 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 25.0 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.74 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 25.0 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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