α-Ecdysone
(Synonyms: 蜕皮激素; α-Ecdysone) 目录号 : GC45204
蜕皮激素（α-蜕皮激素）是一种存在于昆虫和植物中的类固醇蜕皮激素，可激活盐皮质激素受体（MR），从而导致肾小球疾病。
Cas No.:3604-87-3
Sample solution is provided at 25 µL, 10mM.
Ecdysone (α-ecdysone) is a steroidal molting hormone that exists in insects and plants and activates mineralocorticoid receptor (MR), leading to glomerular diseases[1]. Ecdysone is also an essential regulator of developmental transitions, including molting and metamorphosis in insects[2].
Ecdysone (0.1, 1, 5, and 10μM for 24h) significantly downregulated the key proteins of the TLR-pathways such as TLR-4, MYD88, IKK-α and IKK-ϒ in RAW 264.7 cells. These proteins were associated with inflammation. Therefore, ecdysone could suppress the TLR pathway to protect cells from inflammation[3].
Ecdysone treatment (6µg/g/d) resulted in evident mesangial deposition of fibronectin and significant reduction in the expression of podocyte-specific molecules such as synaptophysin in male C57BL/6 mice. These phenomena indicated that ecdysone treatment caused glomerulosclerosis and podocyte injury[4].
References:
[1]. Lu M, Wang P, Ge Y, Dworkin L, Brem A, Liu Z, et al. Activation of mineralocorticoid receptor by ecdysone, an adaptogenic and anabolic ecdysteroid, promotes glomerular injury and proteinuria involving overactive GSK3beta pathway signaling. Sci Rep. 2018;8(1):12225. Epub 20180815. doi: 10.1038/s41598-018-29483-7. PubMed PMID: 30111886.
[2]. Xu T, Jiang X, Denton D, Kumar S. Ecdysone controlled cell and tissue deletion. Cell Death Differ. 2020;27(1):1-14. Epub 20191119. doi: 10.1038/s41418-019-0456-9. PubMed PMID: 31745213.
[3].Bhardwaj M, Mamadalieva NZ, Chauhan AK, Kang SC. alpha-Ecdysone suppresses inflammatory responses via the Nrf2 pathway in lipopolysaccharide-stimulated RAW 264.7 cells. Int Immunopharmacol. 2019;73:405-13. Epub 20190529. doi:10.1016/j.intimp.2019.05.038. PubMed PMID: 31152978.
[4]. Lu M, Wang P, Zhou S, Flickinger B, Malhotra D, Ge Y, et al. Ecdysone Elicits Chronic Renal Impairment via Mineralocorticoid-Like Pathogenic Activities. Cell Physiol Biochem. 2018;49(4):1633-45. Epub 20180918. doi: 10.1159/000493499. PubMed PMID: 30227391.
蜕皮激素（α-蜕皮激素）是一种存在于昆虫和植物中的类固醇蜕皮激素，可激活盐皮质激素受体（MR），从而导致肾小球疾病[1]。蜕皮激素也是昆虫发育转变的重要调节因子，包括蜕皮和变态[2]。
蜕皮激素（0.1、1、5和10μM，持续24小时）在RAW 264.7细胞中显著下调TLR通路的关键蛋白，例如TLR-4、MYD88、IKK-α和IKK-ϒ。这些蛋白与炎症发生有关。因此，蜕皮激素可以抑制TLR通路，从而保护细胞免受炎症影响[3]。
蜕皮激素治疗（6μg/g/d）会导致雄性 C57BL/6 小鼠的纤连蛋白在系膜处明显沉积以及足细胞特异性分子（例如突触素）的表达显著减少。这些现象表明，蜕皮激素治疗会造成肾小球硬化和足细胞损伤[4]。
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Cell experiment [1]: |
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Cell lines |
RAW 264.7 cells |
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Preparation method |
α-Ecdysone was dissolved in 5% DMSO and cells were treated with several concentrations of α-ecdysone (0.1, 1, 5 and 10μM) for 24h. |
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Reaction Conditions |
0.1, 1, 5 and 10μM for 24h |
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Applications |
In RAW 264.7 cells , α-ecdysone significantly enhanced lysosomal activity in a concentration dependent fashion. |
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Animal experiment [2]: |
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Animal models |
Male C57BL/6 mice |
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Preparation method |
Male C57BL/6 mice aged 10 weeks received a daily subcutaneous injection of α-ecdysone at 6μg/g/d. After 14 days of treatment, mice were euthanized and kidneys were collected for examinations. |
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Dosage form |
6μg/g/d, subcutaneous injection |
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Applications |
In vivo, daily treatment of mice with α-ecdysone increased cell apoptosis in the kidney, impaired renal function and elicited early signs of renal fibrogenesis. |
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References: [1]. Bhardwaj M, Mamadalieva NZ, Chauhan AK, Kang SC. alpha-Ecdysone suppresses inflammatory responses via the Nrf2 pathway in lipopolysaccharide-stimulated RAW 264.7 cells. Int Immunopharmacol. 2019;73:405-13. Epub 20190529. doi:10.1016/j.intimp.2019.05.038. PubMed PMID: 31152978. [2]. Lu M, Wang P, Zhou S, Flickinger B, Malhotra D, Ge Y, et al. Ecdysone Elicits Chronic Renal Impairment via Mineralocorticoid-Like Pathogenic Activities. Cell Physiol Biochem. 2018;49(4):1633-45. Epub 20180918. doi:10.1159/000493499. PubMed PMID: 30227391. |
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| Cas No. | 3604-87-3 | SDF | |
| 别名 | 蜕皮激素; α-Ecdysone | ||
| 化学名 | (5β)-2β,3β,14,22R,25-pentahydroxy-cholest-7-en-6-one | ||
| Canonical SMILES | O=C1[C@]2([H])C[C@@H](O)[C@@H](O)C[C@]2(C)[C@]3([H])C([C@@](CC[C@@H]4[C@H](C)[C@H](O)CCC(C)(O)C)(O)[C@]4(C)CC3)=C1 | ||
| 分子式 | C27H44O6 | 分子量 | 464.6 |
| 溶解度 | DMF: 2 mg/mL,DMSO: 0.1 mg/mL,Ethanol: 20 mg/mL,Ethanol:PBS (pH 7.2)(1:2): 0.3 mg/mL | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1524 mL | 10.7619 mL | 21.5239 mL |
| 5 mM | 0.4305 mL | 2.1524 mL | 4.3048 mL |
| 10 mM | 0.2152 mL | 1.0762 mL | 2.1524 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet