PRX-08066
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
| 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 |
| SDF | Download SDF |
| 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 | 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。 |
化学结构
