| 中文名称: | Palosuran | ||||
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| 英文名称: | Palosuran | ||||
| 别名: | Palosuran ACT058362; 1-(2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl)-3-(2-methylquinolin-4-yl)urea | ||||
| CAS No: | 540769-28-6 | 分子式: | C25H30N4O2 | 分子量: | 418.54 |
| CAS No: | 540769-28-6 | ||||
| 分子式: | C25H30N4O2 | ||||
| 分子量: | 418.54 | ||||
基本信息
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产品编号： |
P10394 |
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产品名称： |
Palosuran |
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CAS: |
540769-28-6 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
418.54 |
-20℃ |
1个月 |
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化学名： |
1-(2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl)-3-(2-methylquinolin-4-yl)urea |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.3893mL |
11.9466mL |
23.8932mL |
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5mM |
0.4779mL |
2.3893mL |
4.7786mL |
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10mM |
0.2389mL |
1.1947mL |
2.3893mL |
生物活性
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产品描述 |
一种尾加压素II受体拮抗剂。 |
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靶点 |
3.6 nM (human urotensin II receptor) |
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体外研究 |
Palosuran (8h) inhibits 125I-U-II binding to human UT receptor,with IC50s of 46.2nM on TE 671 cells and 86nM on recombinant CHO cells.Palosuran inhibits Ca2+mobilization in response to human U-II in CHO cells expressing human and rat UT receptor with IC50s of 17 and>10000nM,respectively.Palosuran (0.12-10000nM;20 min) inhibits human U-II induced MAPK phosphorylation in a dose-dependent manner in recombinant CHO cells,with an IC50 of 150nM.Phentolamine (1mg/kg;i.v.) produces hypotension and tachycardia in rats. |
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体内研究 |
ACT-058362 (10mg/kg/h;i.v.) fully prevents the decrease in renal blood flow after ischemia in rats without decreasing blood pressure.Palosuran (300mg/kg/d;p.o.for 16 weeks) improves the survival,increases insulin,and slows the increase in glycemia,glycosylated hemoglobin,and serum lipids in streptozotocin-induced diabetic rats. |
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Animal Model: |
Male Wistar rats with renal ischemia and reperfusion |
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Dosage: |
20mg/kg/h for 135 min |
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Administration: |
I.v.(continuous infusion) for 135 min |
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Result: |
Restored renal blood flow to baseline values at 30 min after reperfusion and by 60 min increased renal blood flow by 12% above baseline values.Did not significantly alter mean arterial blood pressure (MAP) and heart rate (HR). |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
