|Description||PRX 08066, a selective 5-hydroxytryptamine receptor 2B(5-HT2BR) antagonist, causes selective vasodilation of pulmonary arteries. Its IC50 value is 3.4 nM. It can potentially inhibit the pathologic 5-HT-induced vascular muscularization and is developed to treat for pulmonary arterial hypertension (PAH). It reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats. It shows effects on the vascular muscularization induced by 5-HT in the in vitro studies. It inhibits 5-HT-induced mitogen-activated protein kinase activation and markedly reduces thymidine incorporation in Chinese hamster ovary cells expressing the human 5-HT2BR in vitro. It decreases level of transcripts of TGFβ1, FGF2 and TPH1 in KRJ-I cells. It significantly reduces peak pulmonary artery pressure at 50 mg/kg and 100 mg/kg compared with monocrotaline control rats. It also significantly attenuates the elevation in pulmonary artery pressure and RV hypertrophy and maintains cardiac function. It reduces the hypoxia-dependent increase in right ventricular systolic pressure in both rats and mice without affecting the systemic mean arterial pressure in the animals. It is also found to have anti-proliferative and anti-fibrotic effects. It was developed by Allergan company and is in clinical phase 2 with no progression.|
|Synonyms||PRX-08066; PRX 08066; PRX08066. 5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]methyl]-2-fluorobenzonitrile|
|Solubility||DMSO: ≤ 7 mg/mL (Need ultrasonic)|
|Application||PRX 08066 can potentially inhibit the pathologic 5-HT-induced vascular muscularization and is developed to treat for pulmonary arterial hypertension (PAH). It is also found to have anti-proliferative and anti-fibrotic effects.|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
|Quantity||Grams to Kilograms|
|Boiling Point||579.9±50.0 °C | Condition: Press: 760 Torr|
|Density||1.44±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr|
|Current Developer||PRX 08066 was developed by Allergan company and is in clinical phase 2 with no progression.|
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