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PRX-08066

更新时间:2025-08-28 08:52:53 采购访问:37次

常用名 PRX-08066游离态 CAS号 866206-54-4
价格 ¥2053.0/5mg ¥需询单/1g ¥需询单/1g ¥需询单/1g 纯度 98.0%
备货期 1天 库存 现货
产品网页 http://www.aladdin-e.com/zh_cn/P127869.html
 产品详情(用途,包装等)
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

上海阿拉丁生化科技股份有限公司 认证供应商

认证状态:已认证供应商
商品数:165907件
电话:400-6206333-1
地址:上海市新金桥路36号财富中心16楼
地区: 上海市 上海市 浦东新区
联系人:阿拉丁
联系人电话:400-620-6333
邮件:li.zg@aladdin-e.com
网址:https://www.aladdin-e.com
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阿拉丁(A股科创板上市企业,股票代码:688179) 是科研服务领域的领先供应商与制造商,拥有科学服务领域领导品牌:阿拉丁。核心业务涵盖高端化学与生化试剂、生命科学、小分子及化合物库及材料科学四大领域,并自主拥有“芯硅谷”实验耗材品牌,依托电商平台实现线上主导的销售模式 。产品广泛服务于985/211高校、科研院所及生物医药、化工材料等领域220余家A股上市公司。
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参考价格:$290/10mM*1mLinDMSO
其他供应商价格:
2024-07-15 PRX-08066
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2023-03-21 PRX-08066
价格:¥需询单
2021-02-06 PRX-08066
价格:¥2089.0

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