2. NF-κB Metabolic Enzyme/Protease Immunology/Inflammation MAPK/ERK Pathway Stem Cell/Wnt
  3. RANKL/RANK Reactive Oxygen Species (ROS) NF-κB p38 MAPK ERK JNK MMP
  4. RANKL-IN-1

RANKL-IN-1 是一种选择性核因子-κB 配体受体激活剂 (RANKL) 抑制剂，其 KD 值为 7.6 μM。RANKL-IN-1 对破骨细胞生成具有抑制活性和选择性，其 IC50 值为 0.07 μM，SI 为 82.57。ANKL-IN-1 直接与 RANKL 结合，并阻断 RANKL 诱导的 NF-κB 和 MAPK 通路的激活。RANKL-IN-1 可用于代谢性疾病的研究，如骨质疏松症。

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RANKL-IN-1

RANKL-IN-1 Chemical Structure

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RANKL-IN-1 相关抗体

Top Publications Citing Use of Products

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

查看 JNK 亚型特异性产品:

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JNK1 JNK2 JNK3 JNK

查看 MMP 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RANKL-IN-1 is a selective and orally active Receptor Activator of Nuclear Factor-κ B Ligand (RANKL) inhibitor with a KD value of 7.6 μM. RANKL-IN-1 exhibits inhibitory activity and selectivity against osteoclastogenesis with an IC50 value of 0.07 μM and SI of 82.57. RANKL-IN-1binds directly to RANKL and blocks the RANKL-induced activation of the NF-κB and MAPK pathways. RANKL-IN-1 can be used for the research of metabolic disease, such as osteoporosis[1].

IC50 & Target[1]

MMP-9

 

体外研究
(In Vitro)

RANKL-IN-1 (Compound 19u) (50-400 nM, 4 days) 在 RAW264.7 细胞中无明显细胞毒性[1]。
RANKL-IN-1 (50-400 nM, 4 days) 在 RAW264.7 细胞中可抑制 RANKL 诱导的破骨细胞生成，且不影响成骨细胞分化[1]。
RANKL-IN-1 (50-400 nM, 4 days) 能降低 RAW264.7 细胞中 RANKL 诱导的活性氧 (ROS) 水平，并抑制骨吸收[1]。
RANKL-IN-1 (50-400 nM, 4 days) 可抑制 RAW264.7 细胞中与 RANKL 诱导的破骨细胞分化相关的蛋白表达[1]。

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

RANKL-IN-1 相关抗体:

Immunofluorescence[1]

Cell Line: RAW264.7 cells
Concentration: 50, 100, 200 and 400 nM
Incubation Time: 4 days
Result: Decreased the size of the F-actin ring.
Reduced ROS levels.

Western Blot Analysis[1]

Cell Line: RAW264.7 cells
Concentration: 50, 100, 200 and 400 nM
Incubation Time: 4 days
Result: Downregulated the protein expression of TRAF6 and phosphorylation of p65, p38, ERK and JNK.
Downregulated the activity of the c-Fos/NFATc1 signaling and inhibited the expression of CTSK and MMP-9.
体内研究
(In Vivo)

RANKL-IN-1 (Compound 19u) (0.313-1.25 μg/mL, 96 h) 减轻了斑马鱼骨质疏松模型中的骨丢失[1]。
RANKL-IN-1 (0.5-2 mg/kg，口服，每 2 天一次，持续 11 周) 可防止卵巢切除诱导的骨质疏松小鼠模型中的全身性骨丢失[1]。

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

Animal Model: Zebrafish osteoporosis models[1]
Dosage: 0.313, 0.625 and 1.25 μg/mL
Administration: 96 h
Result: Increased zebrafish skull bone mass.
Animal Model: Ovariectomy-induced osteoporosis mice models[1]
Dosage: 0.5, 1 and 2 mg/kg
Administration: Orally administration, every 2 days for 11 weeks
Result: Increased the bone mineral density, bone volume fraction, trabecular number and the trabecular thickness.
Reduced the trabecular separation and expanded the marrow cavity and trabecular spacing.
Reduced total cholesterol and triglyceride levels and increased high-density lipoprotein cholesterol levels.
Had no significant changes in ALT, AST and BUN levels.
分子量

621.90

Formula

C40H55N5O
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

RANKL-IN-1 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 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

RANKL-IN-1RANKL/RANKReactive Oxygen Species (ROS)NF-κBp38 MAPKERKJNKMMPNuclear factor-κBNuclear factor-kappaBExtracellular signal regulated kinasesc-Jun N-terminal kinaseMatrix metalloproteinasesRANKLMAPKOsteoporosisRAW264.7ROSInhibitorinhibitorinhibit

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