2. Nrf2 activator-23

Nrf2 activator-23 是一种口服有效的 Keap1 结合剂及 Nrf2 激活剂，对 Keap1 及其 Kelch 功能域的 KD 分别为 28.68 nM 和 54.55 nM。Nrf2 activator-23 破坏 Keap1-Nrf2 相互作用，减少 Nrf2 的泛素化与降解，并激活 Nrf2 信号通路。Nrf2 activator-23 可抑制 RANKL 诱导的破骨细胞形成、骨吸收活性、ROS 生成以及 MAPK、NF-κB 信号通路的激活，同时降低破骨细胞特异性基因与蛋白的表达。Nrf2 activator-23 可在体内减轻骨丢失并减少破骨细胞形成，且不影响成骨细胞的分化与矿化。Nrf2 activator-23 可用于骨质疏松症的研究。

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Nrf2 activator-23

Nrf2 activator-23 Chemical Structure

CAS No. : 3109883-60-2

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Nrf2 activator-23 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nrf2 activator-23 is an orally active Keap1 binder and Nrf2 activator, with KD values of 28.68 nM and 54.55 nM for Keap1 and its Kelch domain, respectively. Nrf2 activator-23 disrupts the Keap1-Nrf2 interaction, reduces ubiquitination and degradation of Nrf2, and activates the Nrf2 signaling pathway. Nrf2 activator-23 inhibits RANKL-induced osteoclast formation, bone resorptive activity, ROS production, and activation of the MAPK and NF-κB signaling pathways, while downregulating the expression of osteoclast-specific genes and proteins. Nrf2 activator-23 attenuates bone loss and reduces osteoclast formation in vivo without affecting osteoblast differentiation and mineralization. Nrf2 activator-23 can be used for the research of osteoporosis[1].

体外研究
(In Vitro)

Nrf2 activator-23 (compound 5c) (1 μM; 4-7 d) 可抑制 RAW264.7 细胞中 RANKL 诱导的破骨细胞分化，处理 7 天时的 IC50 为 0.499 μM[1]。
Nrf2 activator-23 (0.5-2 μM; 7 d) 可呈剂量依赖性地破坏 RANKL 刺激的骨髓巨噬细胞 (BMMs) 中 F-肌动蛋白环的形成、减小破骨细胞体积并降低单个破骨细胞的细胞核数量，处理时间为 7 天[1]。
Nrf2 activator-23 (0.5-2 μM; 7 d) 可呈剂量依赖性地抑制经 RANKL 刺激的 BMMs 的骨吸收作用，处理 7 天后，在 2 μM 浓度下可实现近乎完全的抑制[1]。
Nrf2 activator-23 (0.5-2 μM；7 d) 可呈剂量依赖性下调 RANKL 刺激的 BMM 中破骨细胞分化及功能关键基因 (C-Fos、MMP-9、TRAP、NFATc1、CTSK、DC-STAMP) 的 mRNA 表达水平[1]。
Nrf2 activator-23 (0.5-2 μM; 4 d) 可呈剂量依赖性下调经 RANKL 刺激的骨髓巨噬细胞 (BMMs) 中破骨细胞分化及功能关键标志物 (NFATc1、MMP-9、C-Fos、CTSK) 的蛋白表达[1]。
Nrf2 activator-23 (0.5-2 μM; 48 h) 呈剂量依赖性抑制 RANKL 诱导的骨髓巨噬细胞 (BMMs) 内的细胞内及线粒体 ROS 生成，处理时长为 48 h[1]。
Nrf2 activator-23 (1 μM; 48 h) 可降低 BMMs 中 Nrf2 的泛素化水平，抑制其蛋白酶体降解[1]。
Nrf2 activator-23 (1 μM；6 h) 可在预处理 6 h 后抑制 RANKL 诱导的 BMMs 中 MAPK (p38、ERK、JNK) 和 NF-κB (p65、IκBα) 信号通路的激活[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Nrf2 activator-23 相关抗体:

Real Time qPCR[1]

Cell Line: RANKL-induced mouse bone marrow macrophages (BMMs)
Concentration: 0.5-2 μM
Incubation Time: ~7 days (until osteoclast formation)
Result: Dose-dependently reduced the mRNA expression of all tested osteoclast-specific genes.
Reduced C-Fos, MMP-9, TRAP, NFATc1, and CTSK expression to <20% of the RANKL-induced control, and DC-STAMP expression to ~30% of the control at 2 μM.

Western Blot Analysis[1]

Cell Line: RANKL-induced mouse bone marrow macrophages (BMMs)
Concentration: 0.5-2 μM
Incubation Time: 4 days
Result: Dose-dependently reduced the protein expression of NFATc1, MMP-9, C-Fos, and CTSK compared to the RANKL-induced control.
Reduced NFATc1 and C-Fos expression to <50% of the control, and MMP-9 and CTSK expression to ~40% of the control at 2 μM.

Western Blot Analysis[1]

Cell Line: RANKL-induced mouse bone marrow macrophages (BMMs)
Concentration: 1 μM
Incubation Time: 6 h pre-incubation, followed by RANKL stimulation for up to 60 min
Result: Attenuated RANKL-induced phosphorylation of p38, ERK, JNK, p65, and IκBα in a time-dependent manner.
Reduced p38, ERK, and JNK phosphorylation to ~60-70% of the control, and p65 and IκBα phosphorylation to ~50-60% of the control at 10 min post-RANKL stimulation.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t Cmax T1/2 Bioavailability
Mice[1] 10 mg/kg p.o. 5069 ng·h/mL 223 ng/mL >24 h 9.4 %
体内研究
(In Vivo)

Nrf2 activator-23 (compound 5c) (10 mg/kg；灌胃；每隔 1 天给药 1 次；持续 8 周) 可有效缓解雌性 C57BL/6J 小鼠卵巢切除诱导的骨丢失，效果与 Alendronate sodium hydrate (HY-11101) 相当[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (7-week-old female, ovariectomized)[1]
Dosage: 10 mg/kg
Administration: p.o.; every other day; 8 weeks
Result: Increased bone volume/total bone volume (BV/TV), trabecular number (Tb.N), and trabecular thickness (Tb.Th), while decreasing trabecular spacing (Tb.Sp) compared to OVX controls.
Prevented the decrease in bone surface (BS) caused by ovariectomy.
Markedly reduced the increase in osteoclast surface/bone surface (Oc.S/BS) ratio induced by OVX.
Promoted gene expression of Nfe2l2 and Cat.
Showed no obvious toxicity, with no differences in body weight or organ histology (heart, liver, spleen, lung, kidney).
分子量

423.34

Formula

C23H17FO2Se
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Nrf2 activator-23 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nrf2 activator-233109883-60-2osteoporosisosteoblastsNrf2 signaling pathwayKelch domainKeap1osteoclastsRAW264.7 cellsBMMsRANKLNrf2Inhibitorinhibitorinhibit

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