| CAS NO: | 866206-54-4 |
| 包装: | 5mg |
| 市场价: | 1900元 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 401.89 |
| Cas No. | 866206-54-4 |
| Formula | C19H17ClFN5S |
| Solubility | ≥20.1 mg/mL in DMSO with ultrasonic; insoluble in H2O; ≥2.85 mg/mL in EtOH with gentle warming |
| Chemical Name | 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
PRX-08066是5-羟色胺2B受体(5-HT2BR)的选择性拮抗剂,其Ki值为3.4 nM[1].
据发现,PRX-08066选择性地引起肺动脉血管舒张,被研发用于治疗肺动脉高压(PAH).体外研究表明,PRX-08066对5-HT诱导的血管肌化有效.PRX-08066可以抑制5-HT诱导的丝裂原活化蛋白激酶活化,其IC50值为12 nM.在表达人5-HT2BR的CHO细胞中,PRX-08066显著减少胸苷掺入,其IC50值为3 nM.在小鼠和大鼠模型中,PRX-08066逆转右心室收缩压的缺氧依赖性增加.此外,PRX-08066具有抗增殖和抗纤维化作用.PRX-08066能够抑制5-羟色胺分泌\ERK1/2磷酸化以及促纤维化生长因子合成.PRX-08066可以抑制小肠神经内分泌肿瘤细胞系KRJ-1增殖,其IC50值为4.6 nM[1,2].
参考文献：
[1] Porvasnik S L, Germain S, Embury J, et al. PRX-08066, a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats. Journal of Pharmacology and Experimental Therapeutics, 2010, 334(2): 364-372.
[2] Svejda B, Kidd M, Giovinazzo F, et al. The 5-HT2B receptor plays a key regulatory role in both neuroendocrine tumor cell proliferation and the modulation of the fibroblast component of the neoplastic microenvironment. Cancer, 2010, 116(12): 2902-2912.
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