Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PRX-08066 Maleic acid 是一种选择性 5-HT2B 受体拮抗剂,IC50 为 3.4 nM,可防止 MCT 大鼠模型中肺动脉高压的严重程度。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 5,970 | 6-8周 | ||
50 mg | ¥ 7,919 | 6-8周 | ||
200 mg | ¥ 18,239 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,854 | 6-8周 |
PRX-08066 Maleic acid 的其他形式现货产品:
产品描述 | PRX-08066 Maleic acid is a selective 5-HT2B receptor antagonist with IC50 of 3.4 nM, prevents the severity of pulmonary arterial hypertension in the MCT rat model. Phase 2. |
靶点活性 | 5-HT2B:3.4 nM |
体外活性 | 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] |
体内活性 | 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] |
细胞实验 | 5×103 cells/mL, seeds in 96-well plates at 100 μL (4 plates/experimental condition) are stimulated with PRX-08066 (0.1 μM to 100 nM: n = 6 wells/concentration). After 24 hours, mitochondrial activity is measured after adding MTT (3-[4,5-dimethylthiazol-2-ly]-2.5-diphenyltetrazolium bromide: 0.5 mg/mL per well) for 3 hours. The optical density is read photospectrometrically at 595 nm using a microplate reader. 29 Results are normalized to control (unstimulated cells) and the effective half-maximal concentrations calculated.(Only for Reference) |
分子量 | 517.96 |
分子式 | C19H17ClFN5S·C4H4O4 |
CAS No. | 866206-55-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 91 mg/mL (175.7 mM)
H2O: 95 mg/mL (183.4 mM)
DMSO: 96 mg/mL (185.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / H2O / DMSO | 1 mM | 1.9307 mL | 9.6533 mL | 19.3065 mL | 48.2663 mL |
5 mM | 0.3861 mL | 1.9307 mL | 3.8613 mL | 9.6533 mL | |
10 mM | 0.1931 mL | 0.9653 mL | 1.9307 mL | 4.8266 mL | |
20 mM | 0.0965 mL | 0.4827 mL | 0.9653 mL | 2.4133 mL | |
50 mM | 0.0386 mL | 0.1931 mL | 0.3861 mL | 0.9653 mL | |
100 mM | 0.0193 mL | 0.0965 mL | 0.1931 mL | 0.4827 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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