| Identification | Back Directory | [Name]
PRX-08066 | [CAS]
866206-55-5 | [Synonyms]
CS-2323
PRX-08066(96%)
PRX-08066 USP/EP/BP
PRX-08066 Maleic acid
5-[[4-[(6-Chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluoro-benzonitrile (2Z)-2-butenedioate (1:1)
Benzonitrile, 5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluoro-, (2Z)-2-butenedioate (1:1) | [Molecular Formula]
C23H21ClFN5O4S | [MDL Number]
MFCD23704188 | [MOL File]
866206-55-5.mol | [Molecular Weight]
517.96 |
| Hazard Information | Back Directory | [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 | [IC 50]
5-HT2B Receptor: 3.4 nM (IC50) |
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