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Dexamethasone acetate.

(Synonyms: 醋酸地塞米松; Dexamethasone 21-acetate; Hexadecadrol acetate)
目录号: PC10747 纯度: ≥98%
IL受体调节剂,Dexamethasone是糖皮质素类甾体化合物,有抗炎和免疫抑制活性。
CAS No. :1177-87-3
商品编号 规格 价格 会员价 是否有货 数量
PC10747-1g 1g ¥658.00 请登录
PC10747-5g 5g ¥3042.00 请登录
PC10747-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥1248.00 请登录
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中文名称
Dexamethasone acetate.
中文别名
醋酸地塞米松;16alpha-甲基-11beta,17alpha,21-三羟基-9alpha-氟孕甾-1,4-二烯-3,20-二酮-21-醋酸酯;21α-乙酰氧基-9α-氟-11β,17α-二羟基-16α-甲基孕甾-1,4-二烯-3,20-二酮;9α-氟-11β,17α,21-三羟基-16α-甲基孕甾-1,4-二烯-3,20-二酮-21-醋酸酯;醋酸氟甲强的松龙;醋酸氟美松;醋酸甲氟烯索;地塞米松醋酸酯;醋酸地塞米松 GMP;醋酸地塞米松原粉;乙酸地塞米松;21-乙酸地塞米松;Dexamethasone 21-Acetate 21-乙酸地塞米松;醋酸地塞米松标准品;醋酸地塞米松原药;醋酸地塞米松中间体;地塞米松醋酸酯 标准品;地塞米松醋酸酯,CP2005,USP,BP,EP;皮炎平 USP标准品;盐酸普鲁卡因;醋酸倍氟美松杂质B(EP) 标准品;地塞米松杂质G;9α-氟-16α-甲基-11β,17α,21-三羟基--1,4-孕甾二烯-3,20-二酮-21-乙酸酯;9α-氟-16α-甲基氢化泼尼松龙-21-乙酸酯;泼尼松龙乙酸酯
英文名称
Dexamethasone acetate
英文别名
dexamethasone-21-acetate;1,4-PREGNADIEN-9-ALPHA-FLUORO-16-ALPHA-METHYL-11-BETA, 17,21-TRIOL-3,20-DIONE 21-ACETATE;9a-fluoro-16a-methyl-11b,17a,21-trihydroxy-1,4-pregnadiene-3,20-dione-21-acetate;9 ALPHA-FLUORO-11 BETA,17 ALPHA,21-TRIHYDRO-16 ALPHA-METHYLPREGNA-1,4-DIENE-3,20-DIONE-21-ACETATE;9ALPHA-FLUORO-16ALPHA-METHYL-11BETA,17ALPHA,21-TRIHYDROXY-1,4-PREGNADIENE-3,20-DIONE-21-ACETATE;9-ALPHA-FLUORO-16-ALPHA-METHYL-11-BETA,17-ALPHA,21-TRIHYDROXY-1,4-PREGNADIENE-3,20-DIONE ACETATE;9ALPHA-FLUORO-16ALPHA-METHYLPREDNISOLONE-21-ACETATE;DEXAMETHASON ACETATE;dexamethasone-17-acetate;DEXAMETHASONE 21-ACETATE;DEXAMETHASONE ACETATE;PREDNISOLONE F ACETATE;,(11beta,16alpha)-;16alpha-Methyl-9alpha-fluoroprednisolone 21-acetate;20-dione,21-(acetyloxy)-9-fluoro-11,17-dihydroxy-16-methyl-pregna-4-diene-3;20-dione,9-fluoro-11-beta,17,21-trihydroxy-16-alpha-methyl-pregna-4-diene-3;9alpha-Fluoro-16alpha-methylprednisolone acetate;9-Fluoro-11,17,21-trihydroxy-16-methylpregna-1,4-diene-3,20-dione21-acetate;9-Fluoro-11,17-dihydroxy-16-methyl-3,20-dioxopregna-1,4-dien-21-yl acetate;9-fluoro-11-beta,17,21-trihydroxy-16-alpha-methylpregna-1,4-diene-3,20-dione;9-Fluoro-11beta,17,21-trihydroxy-16alpha-methylpregna-1,4-diene-3,20-dione 21-acetate;21-O-Acetyl Dexamethasone;9α-Fluoro-11β,17α,21-trihydroxy-16α-methyl-1,4-pregnadiene-3,20-dione 21-Acetate;Dexamethasone EP Impurity G;CID 6551035
Cas No.
1177-87-3
分子式
C24H31FO6
分子量
434.50
包装储存

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

详情描述

IL受体调节剂,Dexamethasone是糖皮质素类甾体化合物,有抗炎和免疫抑制活性。

生物活性

Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.

性状

Solid

IC50 & Target[1][2]

Glucocorticoid receptor

体外研究(In Vitro)

protein-1, nuclear factor-AT, and nuclear factor-kB, leading to the activation and repression of key genes involved in the inflammatory response.
Dexamethasone potently inhibits granulocyte-macrophage colony stimulating factor (GM-CSF) release from A549 cells with EC50 of 2.2 nM. Dexamethasone (EC50=36 nM) induces transcription of the β2-receptor is found to correlate with glucocorticoid receptor (GR) DNA binding and occurred at 10-100 fold higher concentrations than the inhibition of GM-CSF release. Dexamethasone (IC50=0.5 nM) inhibits a 3×κB (NF-κB, IκBα, and I-κBβ), which is associated with inhibition of GM-CSF release.

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

体内研究(In Vivo)

It has previously been reported that treatment with Dexamethasone (Hexadecadrol) at a dose of 2×5 mg/kg efficiently inhibits lipopolysaccharide (LPS)-induced inflammation. In our experimental system, treatment with a single dose of Dexamethasone 10 mg/kg (i.p.) significantly decreases recruitment of granulocytes as well as spontaneous production of oxygen radicals compared with animals expose to LPS and injected with solvent alone (saline). The effects are statistically significant when administered both 1 h before and 1 h after inhalation of LPS. The number of granulocytes in BALF decreased to levels comparable to healthy animals (given an aerosol of water).
Rats treated with Dexamethasone consume less food and weighed less than control rats. Treated rats also weigh less than pair-fed animals though their food intake is similar. Five days of Dexamethasone injection result in a significant increase in both the liver mass (+42%) and the liver to body weight ratio (+65%). The wet weight of gastrocnemius muscle decreases 20% after 5 days of treatment, but it remains unaffected relative to body weight (g/100 g body weight), indicating that muscle weight loss paralleled body weight loss.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : 50 mg/mL (115.07 mM; Need ultrasonic)

H2O : ≥ 1 mg/mL (2.30 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3015 mL 11.5075 mL 23.0150 mL
5 mM 0.4603 mL 2.3015 mL 4.6030 mL
10 mM 0.2301 mL 1.1507 mL 2.3015 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.79 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.79 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.79 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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