| 中文名称: | CID-2858522 | ||||
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| 英文名称: | CID-2858522 | ||||
| 别名: | CID-2858522 国华试剂;1-[3,5-双(1,1-二甲基乙基)-4-羟基苯基]-2-[2-[(3-羟基丙基)氨基]-5,6-二甲基-1H-苯并咪唑-1-基]-乙酮 1-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-[2-[(3-hydroxypropyl)amino]-5,6-dimethyl-1H-benzimidazol-1-yl]-ethanone | ||||
| CAS No: | 758679-97-9 | 分子式: | C28H39N3O3 | 分子量: | 465.63 |
| CAS No: | 758679-97-9 | ||||
| 分子式: | C28H39N3O3 | ||||
| 分子量: | 465.63 | ||||
基本信息
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产品编号： |
C60055 |
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产品名称： |
CID-2858522 |
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CAS: |
758679-97-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
465.63 |
-20℃ |
1个月 |
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化学名： |
1-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-[2-[(3-hydroxypropyl)amino]-5,6-dimethyl-1H-benzimidazol-1-yl]-ethanone |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.1476mL |
10.7381mL |
21.4763mL |
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5mM |
0.4295mL |
2.1476mL |
4.2953mL |
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10mM |
0.2148mL |
1.0738mL |
2.1476mL |
生物活性
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产品描述 |
一种高效的选择性抗原受体介导的NF-κB抑制剂，IC50为70nM。 |
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靶点 |
NF-κB 70 nM (IC50) |
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体外研究 |
CID-2858522 (Compound 1) inhibits antigen receptor-mediated NF-κB with an IC50 of 70nM.CID-2858522 also inhibits testosterone hydroxylase in the presence of human liver microsomes (HLM) and an NADPH generating system with an IC50 of 85μM.In the HEK293 cell line used for primary screening,CID-2858522 suppresses NF-κB reporter gene activity in a concentration-dependent manner,with IC50 ~70nM and with maximum inhibition achieved at 0.25-0.5μM.In contrast,CID2858522 does not inhibit TNF-induced NF-κB-reporter gene activity at concentrations as high as 4μM,thus demonstrating selectivity for the NF-κB pathway activated by PMA/Ionomycin.Cell viability assays indicate that CID-2858522 is not toxic to HEK293 cells at concentrations ≤8μM.CID-2858522 also potently inhibits PMA/Ionomycin-induced NF-κB reporter gene activity in transient transfection assays. |
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体内研究 |
In vivo dose-exposure profiling of CID-2858522 (Compound 1a) is conducted using a small cohort of three male mice.CID2858522 exhibits nonlinear pharmacokinetics,showing higher serum levels at the 0.5h measurement time for the 30mg/kg dose compared to 50mg/kg but displaying typical dose-dependent behavior when measured at t=3h.The increasing accumulation seen at a dose of 50mg/kg may be due to a depot effect created by CYP3A4 inhibition.The cohort exhibits clear signs of morbidity at t=3h at the 50mg/kg dose. |
推荐实验方法(仅供参考)
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细胞实验: |
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Cell viability is estimated based on cellular ATP levels,measured using ATPlite kit.HEK293 cells at a density of 105/mL are seeded at 90μL per well in 96-well white plates and cultured overnight.Compounds (e.g.,CID-2858522;1μM,2μM,3μM,and 4μM) are added (5μL in medium) to wells and cells are cultured for 16h,Finally,50μL ATPlite solution is added to each well and luminescence activity is read using a luminometer. |
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动物实验: |
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Mice Three male mice are subjected to CID-2858522 (single ip doses at 10,30,and 50mg/kg).Blood is drawn at 0.5 and 3h,and subsequent LC/MS analysis of pooled samples is performed to determine the overall blood levels of CID-2858522. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
