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PRX-08066

Catalog No.GC10450

5-HT2BR antagonist

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PRX-08066 Chemical Structure

Cas No.: 866206-54-4

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5mg
$135.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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

Cas No. 866206-54-4 SDF
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
Formula C19H17ClFN5S M.Wt 401.89
Solubility DMSO: 96mg/ml,Ethanol: 91 mg/ml,Water: 95 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.4882 mL 12.4412 mL 24.8824 mL
5 mM 0.4976 mL 2.4882 mL 4.9765 mL
10 mM 0.2488 mL 1.2441 mL 2.4882 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 36 reference(s) in Google Scholar.)

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