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Climbazole
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很棒纯度: 98.23%
货号 T1403Cas号 38083-17-9
别名 甘宝素, BAY-e 6975
Climbazole (BAY-e 6975) 是一种广谱咪唑类抗真菌剂，具有去屑功效。它还是大鼠肝细胞色素 P450 的强诱导剂。
其他形式的 “Climbazole”:
Climbazole
一键复制产品信息 很棒纯度: 98.23%
货号 T1403 别名 甘宝素, BAY-e 6975Cas号 38083-17-9
Climbazole (BAY-e 6975) 是一种广谱咪唑类抗真菌剂，具有去屑功效。它还是大鼠肝细胞色素 P450 的强诱导剂。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 g | ¥ 148 | 现货 | |
| 5 g | ¥ 343 | 现货 | |
| 10 g | ¥ 502 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 99 | 现货 |
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产品介绍
Climbazole AI Summary
Climbazole exhibits a broad spectrum of bioactivity across various biological targets and assays, highlighting its potential for diverse therapeutic applications. It shows inhibitory effects against the Menin-MLL interaction in MLL-related leukemias, malarial parasite plastid, and the Ebola virus entry. Additionally, it demonstrates appreciable inhibition of human tyrosyl-DNA phosphodiesterase 1 (TDP1), gametocytocidal compounds, and Schwann cell intronic element firefly luciferase.
In the context of retinoic acid metabolism, Climbazole functions as a RAMBA, showing potent CYP3A4 inhibition with an IC50 value of 100.0 nM. This activity was further confirmed in pig liver microsomal assays with an IC50 of 47500.0 nM.
The compound also shows antiviral activity against SARS-CoV-2, demonstrating a reduction in cell viability in infected Vero E6 and Caco-2 cells, with inhibition levels of 22.58% at 10 µM and cytotoxicity inhibition percentages of 0.47% and 0.19% at the same concentration.
Further analyses reveal that Climbazole inhibits transglutaminase in human keratinocytes with an IC50 of 4470.0 nM and exhibits significant cytochrome P450 inhibition in rat liver microsomes. It also showcases moderate inhibition against the SARS-CoV-2 3CL-Pro protease at 20µM, with inhibition percentages of 32.01% and 11.3%.
Enzymatic assays indicate that Climbazole inhibits the human HDAC6 enzyme more effectively with a commercial peptide substrate (22.36%) as compared to a custom peptide (5.32%). Additionally, it binds with notable affinity to human SLC6A3, SLC6A2, SLC6A4, and ADORA3, while displaying antagonist activity at human CHRM1 and ADRA1A, and agonist activity at human CHRM1. Finally, it shows inhibition potential against human PTGS1 and ACHE, albeit with higher AC50 values.
Overall, Climbazole's wide-ranging inhibitory activities and binding affinities, across multiple assays and biological targets, support its potential utility in therapeutic interventions against various diseases..
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 | Climbazole (BAY-e 6975) is a broad-spectrum imidazole antifungal agent with anti-dandruff properties. |
| 体外活性 | 在体内外的非常规DNA合成试验中,口服给药的最大耐受量高达200 mg/kg 时,Climbazole没有表现出对大鼠肝脏中DNA的损伤.Climbazole在鼠伤寒沙门氏菌或大肠杆菌Ames试验中没有致突变性,也不诱导人体淋巴细胞中的微核. |
| 体内活性 | Climbazole的MICs范围在<0.06和1 μg/mL之间,实验中值为0.06 μg/mL。Climbazole在体内外都表现出较高的抗Pityrosporum ovale功效,而Pityrosporum ovale可能是产生头皮屑的主要原因。 |
| 别名 | 甘宝素, BAY-e 6975 |
| 分子量 | 292.76 |
| 分子式 | C15H17ClN2O2 |
| CAS No. | 38083-17-9 |
| Smiles | C(OC1=CC=C(Cl)C=C1)(C(C(C)(C)C)=O)N2C=CN=C2 |
| 密度 | 1.321 g/cm3. Temperature:20 °C.;1.317 g/cm3. Temperature:20 °C. |
| 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 | Ethanol: 55 mg/mL (187.87 mM), Sonication is recommended. DMSO: 50 mg/mL (170.79 mM), Sonication is recommended.  H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.83 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/Ethanol
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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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