keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
IRL-1620 is an effective and selective agonist of endothelin receptor type B (ETB) (Ki: 16 pM). 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 IRL-1620 acetate 的水溶性和稳定性通常比游离态更好。
产品描述 | IRL-1620 is an effective and selective agonist of endothelin receptor type B (ETB) (Ki: 16 pM). |
靶点活性 | ETA receptor:19 μM, ETB receptor:16 pM |
体外活性 | IRL-1620 is 60 times more selective for the ETB receptor than ET-3 (KiETA/ KiETB=1,900). IRL-1620 is the most effective and specific ligand for the ETB receptor (KiETA/ KiETB=120,000) as judged by the Ki values for ETA (19 μM) and ETB (16 PM) receptors[1]. |
体内活性 | IRL-1620 improves both acquisition (learning) and retention (memory) on the water maze task and enhances angiogenic and neurogenic remodeling. In rat aorta, IRL-1620 (1-100 nM) enhances cytosolic Ca2+ in the vascular endothelium ([Ca]E) with little effect on resting muscle tone and relaxes the norepinephrine-stimulated tone with an increase in [Ca]E. IRL-1620 (1-100 nM) causes contractions of the guinea pig trachea. For IRL 1620, the effective concentration that produces 30 % of 60 mM KCI-induced contraction is estimated to be 28 nM [1]. Rats treated with IRL-1620 obviously decreases the cognitive impairment induced by Aβ. IRL-1620 treatment enhances the number of blood vessels labeled with VEGF compared to vehicle treatment[2]. IRL-1620 restores analgesic tolerance to morphine and oxycodone, but it does not affect morphine and oxycodone induced decrease in NGF/PI3K expression. IRL-1620 attenuates opioid tolerance without the involvement of NGF/PI3K pathway[3]. |
分子量 | 1820.974 |
分子式 | C86H117N17O27 |
CAS No. | 142569-99-1 |
keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
IRL-1620 142569-99-1 Others IRL1620 IRL 1620 Inhibitor inhibitor inhibit