PRX-08066

产品详情：

更新时间： 2025-08-29 22:48:14

CAS号：866206-54-4

常用名： PRX-08066游离态

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纯度： 98.0%

备货期： 10天

库存： 现货

其他详情（用途，包装）：
用途： PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries. IC50 value: 3.4 nM [1]Target: HT2B receptorin vitro: PRX-08066 inhibits 5-HT-induced mitogen-activated protein kinase activation with IC50 of 12 nM and markedly reduces thymidine incorporation with IC50 of 3 nM in Chinese hamster ovary cells expressing the human 5-HT2BR, which suggests that PRX-08066 can potentially inhibit the pathologic 5-HT-induced vascular muscularization associated with PAH [1]. PRX-08066 inhibits cell proliferation with IC50 of 0.46 nM and with a maximum inhibition of 20% and 5-HT secretion with IC50 of 6.9 nM with a maximum inhibition of 30% in the 5-HT(2B) expressing SI-NET cell line, KRJ-I. PRX-08066 inhibits isoproterenol-stimulated 5-HT release with IC50 of 1.25 nM and a maximum inhibition of 60% in NCI-H720 cells. PRX-08066 (0.5 nM) significantly inhibits ERK phosphorylation in KRJ-I cells. PRX-08066 inhibits TGFβ1, CTGF and FGF2 transcription and secretion in KRJ-I cells. PRX-08066 decreases level of transcripts for Ki67 (84%) as well as Ki67 protein (36.8%) associated with an increase in caspase 3 transcript levels in KRJ-I cells. PRX-08066 decreases level of transcripts of TGFβ1, FGF2 and TPH1 in KRJ-I cells. PRX-08066 significantly increases the number of dead cells (34%) compared with untreated controls in KRJ-I cells. PRX-08066 causes a significant increase in dead/caspase 3 positive cells (76%) and caspase 3 activity (52%) in HEK293 cells [2].in vivo: PRX-08066 (100 mg/kg) treated groups demonstrates less right ventricular hypertrophy and septal flattening than the monocrotaline control group in rats. PRX-08066 significantly reduces peak pulmonary artery pressure at 50 mg/kg and 100 mg/kg compared with monocrotaline control rats. PRX-08066 also significantly reduces right ventricle (RV)/body weight and RV/left ventricle + septum, compared with MCT-treated rats. PRX-08066 significantly attenuates the elevation in pulmonary artery pressure and RV hypertrophy and maintains cardiac function. PRX-08066 significantly 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 [1]. PRX-08066 (100 mg/kg) significantly inhibits both right ventricular systolic pressure and right ventricular/left ventricular +septum weight elevations in rats. PRX-08066 (30 mg/kg) inhibits right ventricular systolic pressure and monocrotaline-induced ERK phosphorylation in whole lung homogenates in rats [3]. 物理化学性质： CAS号：866206-54-4 常用中文名：PRX-08066游离态常用英文名：PRX-08066 分子式：C19H17ClFN5S 分子量：401.888 密度：1.4±0.1 g/cm3 沸点：579.9±50.0 °C at 760 mmHg 熔点：N/A 闪点：304.5±30.1 °C 储存条件：2-8°C，避光，保存于惰性气体中

供应商信息：

公司名：上海化源世纪贸易有限公司推荐

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化源网，2015 年正式成立，是专注服务全球精细化学与生物医药研发领域的专业社群电商平台。
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其他供应商价格：

2022-03-04 价格：￥2053.0 PRX-08066

2023-03-21 价格：￥需询单 PRX-08066

2021-02-06 价格：￥2089.0 PRX-08066

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PRX-08066游离态价格

PRX-08066

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