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Dexamethasone (Synonyms: MK-125, NSC 34521)

カタログ番号GC40775

デキサメタゾンは、グルココルチコイド家族の一員として、マトリックス喪失、炎症および軟骨生存性を含む関節炎に関連する軟骨構造および機能の変化から保護することができます。

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Dexamethasone 化学構造

Cas No.: 50-02-2

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$39.00
在庫あり
100mg
$25.00
在庫あり
500mg
$35.00
在庫あり
1g
$59.00
在庫あり
5g
$143.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 8 publications

Description of Dexamethasone

Dexamethasone, as one member of the glucocorticoid family, can protect against arthritis-related changes in cartilage structure and function, including matrix loss, inflammation and cartilage viability. [1]

In vitro, treatment with 10 nM to 1 μM dexamethasone by 96 h increased the CPPD crystal depositionin in porcine chondrocytes.[5] In vitro experiment it indicated that GR mediates OATP2B1 downregulation induced by dexamethasone (500 nM) in placental trophoblast cells, while farnesoid X receptor mediates BCRP downregulation and MRP4 upregulation.[6] In addition, administration of 25 nM dexamethasone in isolated myogenic satellite cells results in the greatest increase in committed myogenic progenitors. And differentiation of myoblasts into myotubes was greatest with treatment of 25 nM dexamethasone at early differentiation for 5–7days and sustained treatment of 10 nM dexamethasone for 0–7 days.[7]

In vivo, treatment with 2.5 mg/kg/day orally in mice significantly increased the percent of CTLA-4-expressing CD8 T cells.[2] In vivo experiment it shown that collagen-induced mouse was daily intravenously injected of free 1.6 mg/kg Dexamethasone or a single injected of 0.4–4 mg/kg liposomalencapsulated Dexamethasone, the frequency of arthritis occurrence and lower its severity reduced. [3] With 0.1 mg/kg dexamethasone starting 11 d after surgery decrease animal pain response in the affected paw, lowers inflammation and macrophage infiltration and partially rescues PG loss in the joint cartilage in a rat meniscal transection OA model.[4]

References:
[1] Black R, et al. Dexamethasone: chondroprotective corticosteroid or catabolic killer? Eur Cell Mater. 2019 Nov 22;38:246-263.
[2] Giles AJ, et al. Dexamethasone-induced immunosuppression: mechanisms and implications for immunotherapy. J Immunother Cancer. 2018 Jun 11;6(1):51. 
[3] Rauchhaus U, et al. Separating therapeutic efficacy from glucocorticoid side-effects in rodent arthritis using novel, liposomal delivery of dexamethasone phosphate: long-term suppression of arthritis facilitates interval treatment. Arthritis Res Ther. 2009;11(6):R190. 
[4] Ashraf S, et al. Contributions of angiogenesis to inflammation, joint damage, and pain in a rat model of osteoarthritis. Arthritis Rheum. 2011 Sep;63(9):2700-10.
[5] Fahey M, et al. Dexamethasone promotes calcium pyrophosphate dihydrate crystal formation by articular chondrocytes. J Rheumatol. 2009 Jan;36(1):163-9.
[6] Huang W, et al. Dexamethasone induces an imbalanced fetal-placental-maternal bile acid circulation: involvement of placental transporters. BMC Med. 2021 Apr 7;19(1):87.
[7] Larson AA, et al. Effects of Dexamethasone Dose and Timing on Tissue-Engineered Skeletal Muscle Units. Cells Tissues Organs. 2018;205(4):197-207.

Protocol of Dexamethasone

Cell experiment [1]:

Cell lines

The human choriocarcinoma cell line BeWo

Preparation Method

Treated BeWo with 20, 100, and 500 nM of dexamethasone for 5 days, respectively. Cells were cultured in 96-well plates in the presence of dexamethasone at different concentrations (0, 20, 100, and 500 nM) for 5 days. MTS assay was conducted to detect the cytotoxicity of dexamethasone on BeWo cells following the manufacturer’s protocol.

Reaction Conditions

0, 20, 100, and 500 nM, 5 days

Applications

Dexamethasone decreased OATP2B1 and BCRP mRNA expression and increased the MRP4 mRNA expression in a concentration-dependent manner.

Animal experiment [2]:

Animal models

Six to eight week-old female albino C57BL/6 mice

Preparation Method

For intracranial tumor implantation, mice were injected with 1x 103 GL261 cells that were stably transduced with a firefly luciferase-mCherry lentiviral vector. Water-soluble dexamethasone was administered at 1 mg/kg/day by oral gavage.

Dosage form

1 mg/kg/day,oral gavage

Applications

Dexamethasone increased the percentage of CTLA-4-expressing CD4 T cells of tumor-bearing mice in a dose-dependent manner. CTLA-4 blockade enhances survival of dexamethasone-treated mice.

References:

[1]. Huang W, et al. Dexamethasone induces an imbalanced fetal-placental-maternal bile acid circulation: involvement of placental transporters. BMC Med. 2021 Apr 7;19(1):87.

[2]. Giles AJ, et al. Dexamethasone-induced immunosuppression: mechanisms and implications for immunotherapy. J Immunother Cancer. 2018 Jun 11;6(1):51. 

Chemical Properties of Dexamethasone

Cas No. 50-02-2 SDF
同義語 MK-125, NSC 34521
Canonical SMILES O=C1C=C[C@@]2(C)C(CCC3[C@]2(F)[C@@H](O)C[C@@]4(C)[C@@]3([H])C[C@@H](C)[C@]4(O)C(CO)=O)=C1
Formula C22H29FO5 M.Wt 392.5
溶解度 DMSO : ≥ 56 mg/mL (142.69 mM) Ethanol : 8.33 mg/mL (21.23 mM) Storage Store at -20°C,protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Dexamethasone

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1 mg 5 mg 10 mg
1 mM 2.5478 mL 12.7389 mL 25.4777 mL
5 mM 0.5096 mL 2.5478 mL 5.0955 mL
10 mM 0.2548 mL 1.2739 mL 2.5478 mL
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計算

In vivo Formulation Calculator (Clear solution) of Dexamethasone

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Product Documents

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Quality Control

Related Video of Dexamethasone

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Average Rating: 5 ★★★★★ (Based on Reviews and 1 reference(s) in Google Scholar.)

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