| Identification | Back Directory | [Name]
PRX-08066 | [CAS]
866206-54-4 | [Synonyms]
PRX-8066
PRX-08066
PRX08066;PRX 08066
5-[[4-[(6-Chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluorobenzonitrile
Benzonitrile, 5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluoro- | [Molecular Formula]
C19H17ClFN5S | [MDL Number]
MFCD20488005 | [MOL File]
866206-54-4.mol | [Molecular Weight]
401.89 |
| Chemical Properties | Back Directory | [density ]
1.44 | [storage temp. ]
Store at -20°C | [solubility ]
≥20.1 mg/mL in DMSO with ultrasonic; insoluble in H2O; ≥2.85 mg/mL in EtOH with gentle warming | [form ]
solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
PRX 08066 is a class 2 receptor antagonist which may be used in the treatment of pulmonary diseases. | [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. |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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