| CAS NO: | 866206-54-4 |
| 包装: | 5mg |
| 市场价: | 1350元 |
| Cas No. | 866206-54-4 |
| 化学名 | 5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]methyl]-2-fluorobenzonitrile |
| Canonical SMILES | C1CN(CCC1NC2=C3C=C(SC3=NC=N2)Cl)CC4=CC(=C(C=C4)F)C#N |
| 分子式 | C19H17ClFN5S |
| 分子量 | 401.89 |
| 溶解度 | DMSO: 96mg/ml,Ethanol: 91 mg/ml,Water: 95 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | PRX-08066 is a selective antagonist of 5-hydroxytryptamine receptor 2B (5-HT2BR) with Ki value of 3.4nM [1]. PRX-08066 is found to causes selective vasodilation of pulmonary arteries and is developed to treat for pulmonary arterial hypertension (PAH). In the in vitro studies, PRX-08066 shows effects on the vascular muscularization induced by 5-HT. It inhibits 5-HT induced mitogen-activated protein kinase activation with IC50 value of 12nM. In addition, it significantly reduces thymidine incorporation in CHO cells expressing human 5-HT2BR with IC50 value of 3nM. In both mice and rat models, PRX-08066 reverses the hypoxia-dependent increase in right ventricular systolic pressure. Besides that, PRX-08066 is also found to have anti-proliferative and anti-fibrotic effects. It inhibits the secretion of 5-HT, the phosphorylation of ERK1/2 and synthesis of profibrotic growth factor. Moreover, PRX-08066 inhibits the proliferation of the small intestinal neuroendocrine tumor cell line KRJ-I with IC50 value of 4.6nM [1, 2]. References: |
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