Pexacerfont

¥3,800.00¥9,800.00

SKU: MB3002 分类: , 标签:

Pexacerfont
分子式:C₁₈H₂₄N₆O分子量:340.42

简介: Pexacerfont 是一种选择性的促肾上腺皮质激素释放因子 (CRF1) 受体拮抗剂,作用于人 CRF1受体,IC50为 6.1±0.6 nM。
英文名字:BMS-562086
物理性状及指标:
外观:……………………粉末
溶解性:…………………溶于DMSO和乙醇溶液
含量:……………………>98%

储存条件:-20℃,避光防潮密闭干燥

运输条件:2~8℃运输

生物活性(仅来自于公开文献,不保证其有效性)

描述

Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist withIC50of 6.1±0.6 nM for human CRF.

靶点

IC50: 6.1±0.6 nM (human CRF1receptor)

体外

Pexacerfont demonstrates a potent and specific inhibitory effect (IC50=6.1 ± 0.6 nM) toward human CRF1receptor and has greater than 1000-fold lower affinity (IC50>1000 nM) for the CRF-binding protein and biogenic amine receptors

体内

Pexacerfont (BMS-562086) is active in rats (1-10 mg/kg, orally) in the defensive withdrawal and elevated plus maze models of anxiety. After the intravenous bolus dose, the plasma Pexacerfont concentrations exhibited a multiexponential decline in rats, dogs, and chimpanzees. The CLpof Pexacerfont was higher in rats (17.9 mL/kg per min) and dogs (11.6 mL/kg per min) than in chimpanzees (2.0 mL/kg per min). Assuming the value of CLpof Pexacerfont approximates the value of CLbin these three species, Pexacerfont has an estimated hepatic extraction ratio of 0.32, 0.38, and 0.08 in rats, dogs, and chimpanzees, respectively (calculated by dividing CLpby respective hepatic blood flow, 55.2, 30.9, and 25.5 mL/kg per min for rats, dogs, and chimpanzees). The assumption that CLbis equal to CLpis reasonable at least in rats, where the blood to plasma concentration ratio of BMS-562086-equivalent radioactivity was 0.95 at 1 h postdose.

实验参考方法(仅来自公开文献,供参考)

细胞实验:

Caco-2 cells at passage 50 to 60 are seeded on polycarbonate membranes of 24 well Transwell plates at a density of 60,000 cells/cm2. The cells are cultured for 21 to 25 days in culture medium consisting of Dulbecco’s modified Eagle’s medium supplemented with 10% fetal bovine serum, 0.5 mM HEPES, 1% nonessential amino acids, 1% L-glutamine, 100 U/mL penicillin-G, and 100 μg/mL streptomycin. Before the permeability studies, apical (AP) and basolateral (BL) media are replaced with transport buffer (Hanks’ balanced salt solution supplemented with 2% N, N-dimethylacetamide, pH 7.4). AP to BL permeability study is initiated by replacing the AP medium with the transport buffer containing 25 μM BMS-562086. All permeability experiments are performed at 37°C.Transepithelial electrical resistance (TEER) values are measured to assess cell monolayer integrity. TEER values are obtained both at the beginning and at the end of each experiment. Only wells with TEER values between 400 and 500 Ω/cm2throughout the experiment are used in the studies. Mannitol (25 or 100 μM) transport experiments are performed in the same manner as other transport experiments. Mannitol served as a probe of the Caco-2 cell monolayer integrity.

动物实验

Rats
One group of male Sprague-Dawley rats (n=3, 0.34-0.35 kg b.wt.) instrumented with single jugular vein cannulas are designated for oral administration, and a second group of male Sprague-Dawley rats (n=3, 0.34-0.35 kg b.wt.) instrumented with dual jugular vein cannulas are designated for intravenous administration. All rats are fasted for approximately 18 h before use and for 4 h after dosing. Water is provided ad libitum. Pexacerfont (BMS-562086) is administered orally by gavage to three rats at a single dose of 5 mg/kg in 0.5% aqueous methylcellulose. A single intravenous bolus dose of Pexacerfont is administered to three rats at 1 mg/kg in 20% ethanol in saline via the jugular vein cannula. Blood samples (0.2 mL/time point per animal) are collected via the jugular vein cannula for analysis of Pexacerfont at 0, 0.08 (intravenous dose only), 0.17 (intravenous dose only), 0.25, 0.5, 0.75, 1, 2, 4, 8, 12, 24, 48, 72, and 96 h postdose. Plasma is prepared from the blood samples by centrifuging for 10 min at 1000g and 5°C.

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储液配置及储存:DMSO和乙醇中可以溶解,按表中溶解性配置;如溶解困难,可以通过快速搅拌,超声或温和加热(在45-60°C下水浴)。液体稳定性报道的很少,建议现配现用,如需储存,建议:-20℃1-3月;-80℃ 3-6月。

【注意 】
●我司产品为非无菌包装,若用于细胞培养,请提前做预处理,除去热原细菌,否则会导致染菌。
●部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,以上数据仅供参考交流研究之用。

我司所售出产品仅供于科研研究用途(非临床科研研究),每次销售产品行为都适用于我司网上所列明的通用销售条款

规格

25mg, 5mg

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