Palosuran hydrochloride
(Synonyms: ACT-058362 hydrochloride) 目录号 : GC61546
A urotensin II receptor antagonist
Cas No.:2469274-58-4
Sample solution is provided at 25 µL, 10mM.
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Palosuran is an antagonist of the urotensin II receptor (UTR; IC50s = 3.6 and 1,475 nM for CHO cell membranes expressing human and rat recombinant receptors, respectively).1 It inhibits contraction of isolated rat aortic rings induced by urotensin II in a concentration-dependent manner. Palosuran (300 mg/kg twice per day) reduces plasma endothelin-1 , urotensin II, and TGF-β1 levels, as well as the main pulmonary arterial pressure and right ventricular hypertrophy index in a rat model of pulmonary arterial hypertension (PAH) induced by monocrotaline .2 Palosuran (300 mg/kg per day) reduces serum glucose, cholesterol, and triglyceride levels and increases survival in a rat model of diabetes induced by streptozotocin .3 It also decreases albuminuria and global kidney lesion scores in STZ-induced diabetic rats.
1.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 systemJ. Pharmacol. Exp. Ther.311(1)204-212(2004) 2.Onat, A.M., Pehlivan, Y., Turkbeyler, I.H., et al.Urotensin inhibition with palosuran could be a promising alternative in pulmonary arterial hypertensionInflammation36(2)405-412(2013) 3.Clozel, M., Hess, P., Qiu, C., et al.The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic ratsJ. Pharmacol. Exp. Ther.316(3)1115-1121(2006)
| Cas No. | 2469274-58-4 | SDF | |
| 别名 | ACT-058362 hydrochloride | ||
| Canonical SMILES | OC(CC1=CC=CC=C1)(CC2)CCN2CCNC(NC3=CC(C)=NC4=CC=CC=C34)=O.[H]Cl | ||
| 分子式 | C25H31ClN4O2 | 分子量 | 454.99 |
| 溶解度 | DMSO: 50 mg/mL (109.89 mM); Water: 7.14 mg/mL (15.69 mM) | 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 | 2.1979 mL | 10.9893 mL | 21.9785 mL |
| 5 mM | 0.4396 mL | 2.1979 mL | 4.3957 mL |
| 10 mM | 0.2198 mL | 1.0989 mL | 2.1979 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。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet