Palosuran
(Synonyms: ACT-058362) 目录号 : GC17414
A urotensin II receptor antagonist
Cas No.:540769-28-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Palosuran is a potent and specific antagonist of human urotensin-II receptor with IC50 value of 3.6nM [1].
Palosuran is a nonpeptidic, potent and selective antagonist of the urotensin-II receptor. It is selective toward human receptor. The IC50 value of it to rat receptor is 1475nM. The efficacy of palosuran to inhibit Ca2+ mobilization in CHO cells also improved that palosuran is more effective to human UT receptors than to rat UT receptors with IC50 values of 17nM and more than 10μM, respectively. Besides that, palosuran inhibits the phosphorylation of MAPK with IC50 value of 150nM in recombinant CHO cells. Palosuran is selective. It shows no inhibition of other receptors involved in vascular tone regulation such as α-1 adrenoceptor, 5-hydroxytryptamine 2A receptor and endothelin receptor A. Palosuran is used as a pharmacological tool to study the role of endogenous U-II [1, 2].
References:
[1] Carotenuto A, Grieco P, Rovero P, et al. Urotensin-II receptor antagonists. Current medicinal chemistry, 2006, 13(3): 267-275.
[2] Clozel M, Binkert C, Birker-Robaczewska M, et al. Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin system. Journal of Pharmacology and Experimental Therapeutics, 2004, 311(1): 204-212.
| Cas No. | 540769-28-6 | SDF | |
| 别名 | ACT-058362 | ||
| 化学名 | 1-[2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea | ||
| Canonical SMILES | CC1=NC2=CC=CC=C2C(=C1)NC(=O)NCCN3CCC(CC3)(CC4=CC=CC=C4)O | ||
| 分子式 | C25H30N4O2 | 分子量 | 418.53 |
| 溶解度 | ≥ 8.95mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3893 mL | 11.9466 mL | 23.8931 mL |
| 5 mM | 0.4779 mL | 2.3893 mL | 4.7786 mL |
| 10 mM | 0.2389 mL | 1.1947 mL | 2.3893 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。