866206-54-4
Chemical Structure
PRX-08066
- CAS No.: 866206-54-4
- Formula:C19H17ClFN5S
- Molecular Weight:401.89
IUPAC Name: 5-((4-((6-chlorothieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-2-fluorobenzonitrile
InChIKey: IENZFHBNCRQMNP-UHFFFAOYSA-N
SMILES: N#CC1=CC(CN2CCC(NC3=C(C=C(Cl)S4)C4=NC=N3)CC2)=CC=C1F
Biological Activity: PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET)[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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PRX-08066 | 97.46% | PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET). | ||||||||||||||||||||
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References
- [1]. Porvasnik SL, et al. PRX-08066, a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats. J Pharmacol Exp Ther. 2010 Aug;334(2):364-72. [Content Brief]
- [2]. Svejda B, et al. The 5-HT(2B) 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 Jun 15;116(12):2902-12. [Content Brief]
