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PRX-08066

Catalog No.
B1200
5-HT2BR antagonist
Grouped product items
SizePriceStock Qty
5mg
$210.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

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Background

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:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt401.89
Cas No.866206-54-4
FormulaC19H17ClFN5S
Solubility≥20.1mg/mL in DMSO with ultrasonic
Chemical Name5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]methyl]-2-fluorobenzonitrile
SDFDownload SDF
Canonical SMILESC1CN(CCC1NC2=C3C=C(SC3=NC=N2)Cl)CC4=CC(=C(C=C4)F)C#N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

PRX-08066