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Nefazodone hydrochloride
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很棒纯度: 99.86%
货号 T3275Cas号 82752-99-6
别名 萘法唑酮盐酸盐, Serzone, MJ-13754-1, Dutonin, BMY-13754-1, BMY-13754
Nefazodone hydrochloride (Serzone) 是一种强效和选择性的5HT2A 拮抗剂，Ki 为5.8 nM，对 5-HT 和去甲肾上腺素摄取具有中度抑制作用，IC50分别为 290 和 300 nM。它是一种苯哌嗪类抗抑郁药，具有微弱的 α-肾上腺素阻断活性，用于治疗抑郁症、攻击性行为和恐慌症。
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Nefazodone hydrochloride
一键复制产品信息 很棒纯度: 99.86%
货号 T3275 别名 萘法唑酮盐酸盐, Serzone, MJ-13754-1, Dutonin, BMY-13754-1, BMY-13754Cas号 82752-99-6
Nefazodone hydrochloride (Serzone) 是一种强效和选择性的5HT2A 拮抗剂，Ki 为5.8 nM，对 5-HT 和去甲肾上腺素摄取具有中度抑制作用，IC50分别为 290 和 300 nM。它是一种苯哌嗪类抗抑郁药，具有微弱的 α-肾上腺素阻断活性，用于治疗抑郁症、攻击性行为和恐慌症。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 163 | 现货 | |
| 5 mg | ¥ 359 | 现货 | |
| 10 mg | ¥ 578 | 现货 | |
| 25 mg | ¥ 1,090 | 现货 | |
| 50 mg | ¥ 1,630 | 现货 | |
| 100 mg | ¥ 2,420 | 现货 | |
| 200 mg | ¥ 3,580 | 现货 | |
| 500 mg | ¥ 5,730 | 待询 | |
| 1 mL x 10 mM (in DMSO) | ¥ 583 | 现货 |
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产品介绍
Nefazodone hydrochloride AI Summary
Nefazodone hydrochloride exhibits a diverse range of bioactivities, including potential multi-target effects in various biological assays. It shows inhibitory action against multiple targets such as Lamin A Splicing, Tau Fibril Formation, Menin-MLL Interaction, Neuropeptide S Receptor, JMJD2A-Tudor Domain, Nrf2, BAZ2B, vitamin D receptor (VDR), TGF-β, Cell Surface uPA Generation, and human tyrosyl-DNA phosphodiesterase 1 (TDP1). Additionally, it has antiviral properties, notably inhibiting SARS-CoV-2-induced cytotoxicity in Caco-2 and VERO-6 cells, although with varying effectiveness. Specifically, it inhibits SARS-CoV-2 3CL-Pro protease by 5.097% at 20µM and shows 71.74% inhibition of cytotoxicity at 10µM in Caco-2 cells after 48 hours.
The compound also displays antifungal and antibacterial activities against organisms like Candida albicans, Cryptococcus neoformans, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Acinetobacter baumannii, and Staphylococcus aureus MRSA, with inhibition percentages up to 7.83%. In terms of thermal stability, Nefazodone hydrochloride affects protein domains differently, either increasing or decreasing their melting temperatures, indicating both stabilizing and destabilizing effects.
Furthermore, it exhibits variable bioactivity in GPCR beta-arrestin recruitment assays, impacting targets such as ADRB2, AGTR1, ADGRF1, C5AR1, GPR119, CX3CR1, ADRA2A, FFAR4, S1PR1, GLP1R, APLNR, GPR35, and FPR2, with inhibition percentages ranging from negative values to over 100%. It also shows cytotoxic activity against human HepG2 cells with an IC50 value of 14400.0 nM. This diverse bioactivity profile suggests Nefazodone hydrochloride's potential in multiple therapeutic areas and as a tool in biochemical and cellular research..
Note: Summary generated by AI. Data source: ChEMBL 
生物活性
化学信息
储存&溶解度
| 产品描述 | Nefazodone hydrochloride (Serzone) is a serotoninergic modulating antidepressant that is used in therapy of depression, aggressive behavior and panic disorder. |
| 靶点活性 | 5-HT2A receptor:5.8 nM (Ki) |
| 别名 | 萘法唑酮盐酸盐, Serzone, MJ-13754-1, Dutonin, BMY-13754-1, BMY-13754 |
| 分子量 | 506.47 |
| 分子式 | C25H33Cl2N5O2 |
| CAS No. | 82752-99-6 |
| Smiles | n1(c(nn(c1=O)CCCN1CCN(CC1)c1cc(ccc1)Cl)CC)CCOc1ccccc1.Cl |
| 密度 | no data available |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| 溶解度信息 | DMSO: 25 mg/mL (49.36 mM), Sonication is recommended.  | |||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.95 mM), Sonication is recommended. 请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。 | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
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计算器
体内实验配液计算器
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 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / 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 100 μL DMSO （ 母液浓度为 20 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 100 μL DMSO 母液， 添加 400 μL PEG300 混匀澄清， 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。
剂量转换
对于不同动物的给药剂量换算，您也可以参考 更多
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