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Dexamethasone

Dexamethasone

产品编号 T1076   CAS 50-02-2
别名: MK 125, Prednisolone F, NSC 34521, Hexadecadrol, 地塞米松

Dexamethasone (Hexadecadrol) 是一种糖皮质激素受体激动剂和一种 IL 受体调节剂。Dexamethasone 具有抗炎和免疫抑制活性,可诱导自噬。Dexamethasone 抑制 LPS 诱导的巨噬细胞炎症反应。

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Dexamethasone Chemical Structure
Dexamethasone, CAS 50-02-2
规格 价格/CNY 货期 数量
500 mg ¥ 415 现货
1 mL * 10 mM (in DMSO) ¥ 227 现货
产品目录号及名称: Dexamethasone (T1076)
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纯度: 99.91%
纯度: 99.77%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and an IL receptor modulator. Dexamethasone has anti-inflammatory and immunosuppressive activity and induces autophagy. Dexamethasone inhibits LPS-induced inflammatory responses in macrophages.
体外活性 方法:人结直肠癌细胞 LoVo 和 HCT116 用 Dexamethasone (10-300 µM) 处理 72 h,使用 MTT 方法检测细胞生长抑制情况。
结果:Dexamethasone 剂量依赖性地抑制 LoVo 和 HCT116 细胞生长,300 µM Dexamethasone 对细胞生长的抑制率分别为 52.6% 和 58.8%。[1]
方法:急性淋巴性白血病细胞 RS4;11 用 Dexamethasone (100 nM) 处理 24-36 h,使用电子显微镜检查细胞形态。
结果:在 Dexamethasone 处理 24  h 的细胞中,液泡被双膜包围,这是自噬体的特征,并含有膜结构和/或部分内质网或大量细胞质。除了自噬体的出现外,细胞核和细胞形态最初是完整的,这表明自噬体形成先于细胞死亡。Dexamethasone 诱导自噬。[2]
方法:活化的小鼠和人类 T 细胞用 Dexamethasone (0.001-10 μM) 处理 48 h,使用 Flow Cytometry 方法检测 PD-1 的表达。
结果:Dexamethasone 增强小鼠和人活化 T 细胞中 PD-1 的表达。[3]
体内活性 方法:为研究抗炎作用,将 Dexamethasone (1-10 mg/kg) 单次腹腔注射给 LPS 诱导的炎症 C57Bl/6JBom 小鼠。
结果:10 mg/kg Dexamethasone 可显著减少支气管肺泡灌洗液中的中性粒细胞。Dexamethasone 治疗使 TNF-α、IL-1α、IL-1β、IL-6、IL-12p40 和 MIP-1α mRNA 水平显著下调。Dexamethasone 在急性气道炎症中发挥抗炎和抗氧化作用。[4]
方法:为检测体内抗肿瘤活性,将 Dexamethasone (1 mg/kg) 腹腔注射给携带人骨髓瘤肿瘤 OPM2 的 SCID 小鼠,每周五天,持续三周。
结果:Dexamethasone 治疗显著抑制 OPM2 肿瘤的生长,表明在体内具有抗肿瘤活性。[5]
动物实验 NAC was administered at three different doses (10, 100 and 500 mg/kg body weight). At the highest concentration, the acidic pH of the NAC solution was adjusted by adding NaOH. Dexamethasone was administered as a single injection of 1 or 10 mg/kg. Both drugs were dissolved in saline and 400 μl were injected intraperitoneally, either 1 h before or 1 h after LPS exposure. In one experiment, NAC (100 and 500 mg/kg) was injected successively every 4·5 h, starting 1 h before challenge (five injections in total). A control group of LPS-exposed animals were injected intraperitoneally with solvent alone (saline). Intratracheal administration was performed by instillation of 100 μl NAC (50, 100 or 500 mg/kg) or dexamethasone (10 mg/kg) into the lungs of mice anaesthetized with 15 mg/kg Rapinovet (i.v.) [4].
别名 MK 125, Prednisolone F, NSC 34521, Hexadecadrol, 地塞米松
化合物与蛋白结合的复合物

T1076_2

Crystal structure of WT AncGR2-LBD WT bound to dexamethasone and SHP coregulator fragment

分子量 392.46
分子式 C22H29FO5
CAS No. 50-02-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 6 mg/mL (15.28 mM)

DMSO: 73 mg/mL (186 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.548 mL 12.7402 mL 25.4803 mL 63.7008 mL
5 mM 0.5096 mL 2.548 mL 5.0961 mL 12.7402 mL
10 mM 0.2548 mL 1.274 mL 2.548 mL 6.3701 mL
DMSO 20 mM 0.1274 mL 0.637 mL 1.274 mL 3.185 mL
50 mM 0.051 mL 0.2548 mL 0.5096 mL 1.274 mL
100 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.637 mL

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TargetMol Library Books参考文献

1. He J, et al. Dexamethasone affects cell growth/apoptosis/chemosensitivity of colon cancer via glucocorticoid receptor α/NF-κB. Oncotarget. 2017 Jun 28;8(40):67670-67683. 2. Laane E, et al. Cell death induced by dexamethasone in lymphoid leukemia is mediated through initiation of autophagy. Cell Death Differ. 2009 Jul;16(7):1018-29. 3. Xing K, et al. Dexamethasone enhances programmed cell death 1 (PD-1) expression during T cell activation: an insight into the optimum application of glucocorticoids in anti-cancer therapy. BMC Immunol. 2015 Jun 26;16:39. 4. Rocksén D, et al. Differential anti-inflammatory and anti-oxidative effects of dexamethasone and N-acetylcysteine in endotoxin-induced lung inflammation. Clin Exp Immunol. 2000 Nov;122(2):249-56. 5. Kervoëlen C, et al. Dexamethasone-induced cell death is restricted to specific molecular subgroups of multiple myeloma. Oncotarget. 2015 Sep 29;6(29):26922-34. 6. Huang L, Li Q. Notoginsenoside R1 promotes differentiation of human alveolar osteoblasts in inflammatory microenvironment through inhibiting NF‑κB pathway and activating Wnt/β‑catenin pathway[J]. Molecular Medicine Reports. 2020, 22(6): 4754-4762. 7. Zhang, Depeng, et al. Tabersonine attenuates lipopolysaccharide-induced acute lung injury via suppressing TRAF6 ubiquitination[J]. Biochemical pharmacology. 2018 Aug;154:183-192. 8. Sun C, Li X, Guo E, et al. MCP-1/CCR-2 axis in adipocytes and cancer cell respectively facilitates ovarian cancer peritoneal metastasis[J]. Oncogene. 2019: 1-15. 9. Li M, Yu H. Identification of WP1066, an inhibitor of JAK2 and STAT3, as a Kv1. 3 potassium channel blocker[J]. . British Journal of Pharmacology. 2021

TargetMol Library Books文献引用

1. Liu Z, Tan S, Zhou L, et al.SCGN deficiency is a risk factor for autism spectrum disorder.Signal Transduction and Targeted Therapy.2023, 8(1): 1-15. 2. Chen S, Zhou X, Li W, et al.Development of a novel peptide targeting GPR81 to suppress adipocyte-mediated tumor progression.Biochemical Pharmacology.2023: 115800. 3. Xiong W, Jia L, Liang J, et al.Investigation into the anti-airway inflammatory role of the PI3Kγ inhibitor JN-PK1: An in vitro and in vivo study.International Immunopharmacology.2022, 111: 109102. 4. Wang C, Chen R, Zhu X, et al.METTL14 alleviates the development of osteoporosis in ovariectomized mice by upregulating m6A level of SIRT1 mRNA.Bone.2022: 116652. 5. Huang L, Li Q. Notoginsenoside R1 promotes differentiation of human alveolar osteoblasts in inflammatory microenvironment through inhibiting NF‑κB pathway and activating Wnt/β‑catenin pathway. Molecular Medicine Reports. 2020, 22(6): 4754-4762 6. Li M, Yu H. Identification of WP1066, an inhibitor of JAK2 and STAT3, as a Kv1. 3 potassium channel blocker. British Journal of Pharmacology. 2021 Jul;178(13):2617-2631. doi: 10.1111/bph.15441. Epub 2021 May 20. 7. Zhang D, Li X, Hu Y, et al. Tabersonine attenuates lipopolysaccharide-induced acute lung injury via suppressing TRAF6 ubiquitination. Biochemical Pharmacology. 2018, 154: 183-192 8. Ding C, Fu S, Chen X, et al. Epigallocatechin gallate affects the proliferation of human alveolar osteoblasts and periodontal ligament cells, as well as promoting cell differentiation by regulating PI3K/Akt signaling pathway. Odontology. 2021 Jul;109(3):729-740. doi: 10.1007/s10266-021-00597-1. Epub 2021 Mar 6. 9. Chen Q Z, Li Y, Shao Y, et al. TGF-β1/PTEN/PI3K signaling plays a critical role in the anti-proliferation effect of tetrandrine in human colon cancer cells. International Journal of Oncology. 2017, 50(3): 1011-1021 10. Tian S, Wang R, Chen S, et al. Structural Basis for PPARs Activation by the Dual PPARα/γ Agonist Sanguinarine: A Unique Mode of Ligand Recognition. Molecules. 2021, 26(19): 6012.
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Canrenoate potassium AL 082D06 LY404039 Ecdysone Medroxyprogesterone Acetate Prednisolone disodium phosphate Diflorasone Prednisolone

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌临床化合物库 抗癌上市药物库 抗癌药物库 药物功能重定位化合物库 EMA 上市药物库 自噬库 抗感染化合物库 已知活性化合物库 抗病毒库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Dexamethasone 50-02-2 Autophagy Endocrinology/Hormones Immunology/Inflammation Microbiology/Virology Glucocorticoid Receptor Mitophagy IL Receptor SARS-CoV Antibacterial Antibiotic Complement System receptor SARS coronavirus inhibit MK 125 Mitochondrial Autophagy CD18 Prednisolone F CD62L glucocorticoid Inhibitor NSC34521 monocytes NSC 34521 neutrophils Bacterial MK-125 NSC-34521 Hexadecadrol 地塞米松 MK125 CD11b inhibitor

 

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