|
| | PRX-08066 Basic information |
| Product Name: | PRX-08066 | | Synonyms: | 5-[[4-[(6-Chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluoro-benzonitrile (2Z)-2-butenedioate (1:1);PRX-08066 Maleic acid;Benzonitrile, 5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluoro-, (2Z)-2-butenedioate (1:1);PRX-08066(96%);CS-2323;PRX-08066 USP/EP/BP;PRX-08066 (Maleate) | | CAS: | 866206-55-5 | | MF: | C23H21ClFN5O4S | | MW: | 517.9603432 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 866206-55-5.mol |  |
| | PRX-08066 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Powder |
| | PRX-08066 Usage And Synthesis |
| Uses | PRX-08066 Maleic acid is a selective 5-HT2BR antagonist. It has high selectivity over the closely related 5-HT2A and 5-HT2C receptors and other receptor targets. | | Enzyme inhibitor | This selective 5-hydroxytryptamine (serotonin) receptor antagonist (FW = 517.96 g/mol; CAS = 866206-55-5), also named 5-((4-(6-chlorothieno[2,3- d]pyrimidin-4-ylamino)piperidin-1-yl)methyl)-2-fluorobenzonitrile, targets 5-HT2B (IC50 of 3.4 nM), showing high selectivity over the closely related 5-HT2A, 5-HT2C and other receptors and preventing the severity of pulmonary arterial hypertension in the monocrotaline (MCT)-induced rat pulmonary artery hypertension model. PRX-08066 significantly attenuates the elevation in pulmonary artery pressure and right ventricular hypertrophy, thereby improving cardiac function. Targeting the 5-5-HT2B receptor also appears be an effective antiproliferative and antifibrotic strategy for small intestinal neuroendocrine tumors (SI-NETs), because it inhibits tumor microenvironment fibroblasts as well as NET cells. | | target | 5-HT2B |
| | PRX-08066 Preparation Products And Raw materials |
|
