PRX-08066 Maleic acid
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 Maleic acid是一种选择性的5-羟色胺受体2B(5-HT2BR)拮抗剂[1]。
5-HT受体是一类G蛋白偶联受体,在精神分裂症、进食障碍、感知、抑郁症、偏头痛、高血压、焦虑、致幻剂和胃肠道功能障碍等方面扮演重要角色。
在NET细胞系KRJ-I中,PRX-08066抑制5-HT分泌和细胞增殖,降低ERK1/2磷酸化和促纤维化生长因子(TGFβ1、CTGF和FGF2)的合成和分泌。在KRJ-I:HEK293共培养体系中,PRX-08066在KRJ-I细胞系中显著降低5-HT释放以及Ki67、CTGF、TGFβ1和FGF2转录。5-HT自身可刺激HEK293增殖[2]。
PRX-08066在治疗缺氧诱发的肺动脉高压综合征和肺动脉高压的II期临床试验中具有临床前安全性、良好的生物利用度及较低的急性毒性[3]。
在野百合碱(MCT)诱导的PAH雄性大鼠模型中,PRX-08066(100 mg/kg)显著增加右心室射血分数,并在50和100 mg/kg减少峰值PA压力。肺动脉形态学评估表明,PRX-08066显著减少中间壁增厚、管腔闭塞和右心室肥大。另外,PRX-08066减少肺血管重建[1]。
参考文献:
[1]. Porvasnik SL, 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. J Pharmacol Exp Ther, 2010, 334(2): 364-372.
[2]. Svejda B, Kidd M, Giovinazzo F, et al. The 5-HT(2B) receptor plays a key regulatory role in both neuroendocrine tumor cell proliferation and the modulation of the fibroblast component of the neoplastic microenvironment. Cance, 2010, 116(12): 2902-2912.
[3]. Kim SK, Li Y, Abrol R, et al. Predicted structures and dynamics for agonists and antagonists bound to serotonin 5-HT2B and 5-HT2C receptors. J Chem Inf Model, 2011, 51(2): 420-433.
Storage | Store at -20°C |
M.Wt | 517.96 |
Cas No. | 866206-55-5 |
Formula | C19H17ClFN5S·C4H4O4 |
Solubility | Soluble in DMSO |
SDF | Download SDF |
Canonical SMILES | FC(C=C1)=C(C#N)C=C1CN(CC2)CCC2NC3=C(C=C(Cl)S4)C4=NC=N3.O=C(O)/C=C\C(O)=O |
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。 |
Description | PRX-08066 Maleic acid是一种选择性的5-HT2B受体拮抗剂,IC50值为3.4 nM。 | |||||
靶点 | 5-HT2B | |||||
IC50 | 3.4 nM |