CID-2858522
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- CAS号:
- 758679-97-9
- 英文名:
- CID-2858522
- 英文别名:
- 100844;CID-2858522;CID 2858522;CID2858522;1-(3,5-Di-tert-butyl-4-hydroxyphenyl)-2-(2-(3-hydroxypropylamino)-5,6-dimethyl-1H-benzo[d]imid;CID 2858522,Nuclear factor-kappaB,CID-2858522,NF-κB,Nuclear factor-κB,inhibit,CID2858522,Inhibitor;1-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-(2-(3-hydroxypropylaMino)-5,6-diMethyl-1H-benzo[d]iMidazol-1-yl)ethanone;1-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-[2-[(3-hydroxypropyl)amino]-5,6-dimethyl-1H-benzimidazol-1-yl]-ethanone;Ethanone, 1-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-[2-[(3-hydroxypropyl)amino]-5,6-dimethyl-1H-benzimidazol-1-yl]-
- 中文名:
- CID-2858522
- 中文别名:
- CID-2858522,抑制PKC诱导的NF-ΚB活化
- CBNumber:
- CB22642741
- 分子式:
- C28H39N3O3
- 分子量:
- 465.63
- MOL File:
- 758679-97-9.mol
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CID-2858522化学性质
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沸点:
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618.9±65.0 °C(Predicted)
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密度:
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1.12±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: soluble2mg/mL, clear (warmed)
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酸度系数(pKa):
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8.46±0.40(Predicted)
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形态:
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powder
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颜色:
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white to beige
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CID-2858522性质、用途与生产工艺
CID-2858522 是一种高效的选择性抗原受体介导的 NF-κB 抑制剂，IC50 为 70 nM。
CID-2858522 (Compound 1) inhibits antigen receptor-mediated NF-κB with an IC
50
of 70 nM. CID-2858522 also inhibits testosterone hydroxylase in the presence of human liver microsomes (HLM) and an NADPH generating system with an IC
50
of 85 μM. In the HEK293 cell line used for primary screening, CID-2858522 suppresses NF-κB reporter gene activity in a concentration-dependent manner, with IC
50
~70 nM and with maximum inhibition achieved at 0.25-0.5 μM. In contrast, CID-2858522 does not inhibit TNF-induced NF-κB-reporter gene activity at concentrations as high as 4 μM, 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 ≤8 μM. CID-2858522 also potently inhibits PMA/Ionomycin-induced NF-κB reporter gene activity in transient transfection assays.
In vivo dose-exposure profiling of CID-2858522 (Compound 1a) is conducted using a small cohort of three male mice. CID-2858522 exhibits nonlinear pharmacokinetics, showing higher serum levels at the 0.5 h measurement time for the 30 mg/kg dose compared to 50 mg/kg but displaying typical dose-dependent behavior when measured at t=3 h. The increasing accumulation seen at a dose of 50 mg/kg may be due to a depot effect created by CYP3A4 inhibition. The cohort exhibits clear signs of morbidity at t=3 h at the 50 mg/kg dose.
用途
1-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-[2-[(3-hydroxypropyl)amino]-5,6-dimethyl-1H-benzimidazol-1-yl]-ethanone is a selective benzimidazole inhibitor of the antigen receptor-mediated NF-κB a
ctivation pathway.
CID-2858522
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-15530 | CID-2858522
CID-2858522 | 758679-97-9 | 5mg | 1400元 |
| 2024/04/30 | HY-15530 | CID-2858522
CID-2858522 | 758679-97-9 | 10 mM * 1 mLin DMSO | 1540元 |
758679-97-9, CID-2858522 相关搜索:
- NF-kB
- 高端化学
- CID-2858522,抑制PKC诱导的NF-ΚB活化
- 758679-97-9
- CID 2858522,Nuclear factor-kappaB,CID-2858522,NF-κB,Nuclear factor-κB,inhibit,CID2858522,Inhibitor
- Ethanone, 1-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-[2-[(3-hydroxypropyl)amino]-5,6-dimethyl-1H-benzimidazol-1-yl]-
- 100844
- CID 2858522;CID2858522
- 1-(3,5-Di-tert-butyl-4-hydroxyphenyl)-2-(2-(3-hydroxypropylamino)-5,6-dimethyl-1H-benzo[d]imid
- 1-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-[2-[(3-hydroxypropyl)amino]-5,6-dimethyl-1H-benzimidazol-1-yl]-ethanone
- 1-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-(2-(3-hydroxypropylaMino)-5,6-diMethyl-1H-benzo[d]iMidazol-1-yl)ethanone
- CID-2858522