Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Palosuran hydrochloride 540769-28-6(free base) (ACT-058362 hydrochloride) 是一种新型强效特异性人 UT 受体拮抗剂,IC50 为 3.6±0.2 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 574 | 待询 | ||
2 mg | ¥ 1,033 | 待询 | ||
5 mg | ¥ 1,860 | 待询 | ||
10 mg | ¥ 2,890 | 待询 | ||
25 mg | ¥ 4,680 | 待询 | ||
50 mg | ¥ 6,696 | 待询 | ||
100 mg | ¥ 12,053 | 待询 | ||
200 mg | ¥ 21,695 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,860 | 待询 |
Palosuran hydrochloride 540769-28-6(free base) 的其他形式现货产品:
产品描述 | Palosuran hydrochloride 540769-28-6(free base)(ACT-058362 hydrochloride) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM. |
靶点活性 | GPR14:3.6 nM |
体外活性 | Palosuran inhibited 125I-U-II binding to human UT receptors in membrane preparations from CHO cells carrying the human UT receptors almost as potently as cold U-II, with an IC50 of 3.6 ± 0.2 nM. On cells, the inhibitory binding potency of palosuran against human UT receptor was lower than on membranes (IC50 = 46.2 ± 13 nM on TE 671 cells and 86 ± 30 nM on recombinant CHO cells). Compared with the human UT receptor, the binding inhibitory potency of palosuran against the rat UT receptor was lower in membrane preparation (400-fold), as well as in cells (>120-fold) [1]. |
体内活性 | Long-term treatment of streptozotocin-induced diabetic rats with palosuran improved survival, increased insulin, and slowed the increase in glycemia, glycosylated hemoglobin, and serum lipids. Furthermore, palosuran increased renal blood flow and delayed the development of proteinuria and renal damage [2]. Palosuran was rapidly absorbed with maximum plasma concentrations at 1 hour after drug administration. The accumulation factor was 1.7 (geometric mean) (95% confidence interval, 1.3 to 2.1).Palosuran was well tolerated [3]. In mesenteric vessels, palosuran treatment up-regulated expression of RhoA and Rho-kinase, increased Rho-kinase-activity, and diminished nitric oxide (NO)/cyclic guanosine 3',5'-monophosphate (cGMP) signaling. Moreover, palosuran increased renal blood flow, sodium, and water excretion in BDL rats [4]. |
别名 | ACT-058362 hydrochloride |
分子量 | 454.99 |
分子式 | C25H31ClN4O2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: >30 mg/mL
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。
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