2. Stem Cell/Wnt Immunology/Inflammation Metabolic Enzyme/Protease NF-κB
  3. Wnt β-catenin Nuclear Factor of activated T Cells (NFAT) MMP RANKL/RANK
  4. E09241

E09241 是一种口服有效的破骨细胞生成抑制剂。 E09241 通过激活 Wnt/β-catenin，降低 RANKL 诱导的 NFATc1 和 MMP-9 的表达。E09241 可通过上调 OPG 表达来提高 OPG/RANKL 比值，抑制骨吸收、促进骨形成并预防去卵巢相关的骨丢失。E09241 可用于骨质疏松症的研究。

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E09241

E09241 Chemical Structure

CAS No. : 1043110-13-9

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E09241 相关抗体

Top Publications Citing Use of Products

查看 Wnt 亚型特异性产品:

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

E09241 is an orally active osteoclastogenesis inhibitor. E09241 reduces the RANKL-induced expression of NFATc1 and MMP-9 by activating Wnt/β-catenin. E09241 increases the OPG/RANKL ratio by upregulating OPG expression, inhibits bone resorption, promotes bone formation and prevents ovariectomy-related bone loss. E09241 can be used in the research of osteoporosis[1].

体外研究
(In Vitro)

E09241 (24 h) 可上调稳定转染的 U-2OS 细胞中 OPG/RANKL 的比值，其 EC50 为 1.23 μM[1]。
E09241 (0.01-10 μM; 24 h) 可上调 MC3T3-E1 细胞中 OPG mRNA、分泌型蛋白及总蛋白水平，下调 RANKL mRNA 及分泌型蛋白水平[1]。
E09241 (0.01-10 μM; 12-21 days) 可促进 MC3T3-E1 细胞中的成骨细胞分化，ALP 活性、矿化水平以及成骨相关基因 (Runx2、ALP、Bglap) 的表达均升高[1]。
E09241 (0.01-10 μM; 1-3 days) 可通过提升 OPG 水平、降低 RANK 水平，下调 NFATc1 和 MMP-9 的蛋白表达，从而抑制 RANKL 诱导的 RAW264.7 细胞破骨细胞分化[1]。
E09241 (0.01-10 μM; 24-48 h) 可通过提升 β-catenin 水平、降低 DKK1 水平及增强 TCF/LEF 报告基因活性，激活 MC3T3-E1 和 C3H10T1/2 细胞中的经典 Wnt/β-catenin 信号通路[1]。

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

E09241 相关抗体:

Cell Differentiation Assay[1]

Cell Line: MC3T3-E1 mouse calvarial preosteoblasts
Concentration: 0.01-10 μM (ALP activity and gene expression; mineralization)
Incubation Time: 12 days (ALP activity and gene expression); 21 days (mineralization)
Result: Significantly increased ALP activity at 1, 10 μM.
Increased mineralized nodule formation at 1, 10 μM.
Increased Runx2 mRNA levels at 1, 10 μM, ALP mRNA levels at 1, 10 μM, and Bglap mRNA levels at 0.1, 1, 10 μM.
体内研究
(In Vivo)

E09241 (5-20 mg/kg; i.g.; 每日一次共 12 周) 可通过促进骨形成、抑制骨吸收，呈剂量依赖性地减轻去卵巢大鼠的骨质疏松症；在 5 和 20 mg/kg/day 剂量下，大鼠的骨矿物质密度、相对骨体积及骨小梁厚度均得到显著改善[1]。

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

Animal Model: Sprague-Dawley (7-month-old female, 290-310 g, bilateral ovariectomy + intramuscular dexamethasone twice weekly for 4 weeks)[1]
Dosage: 5 mg/kg/day; 20 mg/kg/day
Administration: i.g.; daily; 12 weeks
Result: Reduced trabecular bone loss in a dose-dependent manner.
Increased bone mineral density, relative bone volume, and trabecular thickness in a dose-dependent manner.
Decreased bone surface/bone volume ratio in a dose-dependent manner.
Did not significantly affect trabecular separation and trabecular number.
Improved femur structure compared to untreated ovariectomized rats.
Reduced the number of osteoclasts per bone surface in a dose-dependent manner.
Significantly increased the number of osteoblasts per bone surface at 20 mg/kg/day.
Increased osteoprotegerin levels and the OPG/RANKL ratio in a dose-dependent manner.
Reduced levels of the bone resorption marker CTX-1 in a dose-dependent manner.
Increased levels of the bone formation marker alkaline phosphatase in a dose-dependent manner.
分子量

236.66

Formula

C11H9ClN2O2
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

E09241 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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Help & FAQs
  • 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:

E092411043110-13-9E 09241E-09241Wntβ-cateninNuclear Factor of activated T Cells (NFAT)MMPRANKL/RANKBeta cateninMatrix metalloproteinasesosteoclast differentiationNFATc1osteoprotegerinosteogenic differentiationMMP-9U-2OS cellscanonical Wnt/β-catenin signalingDKK1RANKLInhibitorinhibitorinhibit

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