866206-54-4

Basic information

• Product Name: PRX-08066
• Synonyms: PRX-08066;PRX-8066;5-[[4-[(6-Chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluorobenzonitrile
• CAS NO: 866206-54-4
• Molecular Formula: C₁₉H₁₇ClFN₅S
• Molecular Weight: 401.8881832
• Mol File: 866206-54-4.mol
• Article Data: 2

Chemical Properties

• Appearance: /
• Density: 1.44
• Solubility: ≥20.1 mg/mL in DMSO with ultrasonic; insoluble in H2O; ≥2.85 mg/mL in EtOH with gentle warming
• CAS DataBase Reference: PRX-08066(CAS DataBase Reference)
• NIST Chemistry Reference: PRX-08066(866206-54-4)
• EPA Substance Registry System: PRX-08066(866206-54-4)

Safety Data

• Hazardous Substances Data: 866206-54-4(Hazardous Substances Data)

Usage

Description

PRX-08066 is a class 2 receptor antagonist, a type of drug that blocks the action of specific receptors in the body. It has the potential to be used in the treatment of various pulmonary diseases.

Uses

Used in Pulmonary Disease Treatment:
PRX-08066 is used as a class 2 receptor antagonist for the treatment of pulmonary diseases. Its ability to block specific receptors may help alleviate symptoms and improve the overall health of patients with these conditions.

Biological Activity

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.

InChI:InChI=1S/C19H17ClFN5S/c20-17-8-15-18(23-11-24-19(15)27-17)25-14-3-5-26(6-4-14)10-12-1-2-16(21)13(7-12)9-22/h1-2,7-8,11,14H,3-6,10H2,(H,23,24,25)

Upstream product

• 218301-22-5 2-fluoro-5-formylbenzonitrile 

Relevant articles and documents

New piperidinylamino-thieno[2,3-D] pyrimidine compounds

The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno [2,3-d]pyrimidine compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed.