PRX-08066
- Product Name
- PRX-08066
- CAS No.
- 866206-54-4
- Chemical Name
- PRX-08066
- Synonyms
- PRX-8066;PRX-08066;PRX08066;PRX 08066;5-[[4-[(6-Chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluorobenzonitrile;5-((4-((6-Chlorothieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-2-fluorobenzonitrile;Benzonitrile, 5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluoro-;5-HT Receptor,5-hydroxytryptamine Receptor,Serotonin Receptor,PRX-08066,PRX 08066,PRX08066,inhibit,Inhibitor
- CBNumber
- CB62538815
- Molecular Formula
- C19H17ClFN5S
- Formula Weight
- 401.89
- MOL File
- 866206-54-4.mol
PRX-08066 Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 474171
- Product name
- PRX 08066
- Packaging
- 100mg
- Price
- $1848
- Updated
- 2021/12/16
- Product number
- FP102683
- Product name
- PRX 08066
- Packaging
- 10mg
- Price
- $185
- Updated
- 2021/12/16
- Product number
- CS-0991
- Product name
- PRX-08066
- Purity
- 97.04%
- Packaging
- 5mg
- Price
- $190
- Updated
- 2021/12/16
- Product number
- B1200
- Product name
- PRX-08066
- Packaging
- 5mg
- Price
- $210
- Updated
- 2021/12/16
- Product number
- CS-0991
- Product name
- PRX-08066
- Purity
- 97.04%
- Packaging
- 10mg
- Price
- $280
- Updated
- 2021/12/16
PRX-08066 Chemical Properties,Usage,Production
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.
PRX-08066 Preparation Products And Raw materials
Raw materials
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