Dexamethasone

Dexamethasone (Hexadecadrol) 是一種糖皮質(zhì)ji素受體 (glucocorticoid receptor) 激動劑。Dexamethasone 還顯著降低中性粒細(xì)胞的 CD11b，CD18 和 CD62L 表達(dá)，以及單核細(xì)胞的 CD11b 和 CD18 表達(dá)。Dexamethasone 有潛力用于 COVID-19 的研究。Dexamethasone 在 LPS 誘導(dǎo)的巨噬細(xì)胞炎癥反應(yīng)中，抑制含有炎性 miRNA-155 的外泌體的產(chǎn)生。

貨號：HY-14648
CAS：50-02-2

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號：HY-14648

起訂量：1

規(guī)格:：500mg

價格:：￥500

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產(chǎn)品詳情

Dexamethasone

Dexamethasone (Hexadecadrol) 是一種糖皮質(zhì)ji素受體 (glucocorticoid receptor) 激動劑。Dexamethasone 還顯著降低中性粒細(xì)胞的 CD11b，CD18 和 CD62L 表達(dá)，以及單核細(xì)胞的 CD11b 和 CD18 表達(dá)。Dexamethasone 有潛力用于 COVID-19 的研究。Dexamethasone 在 LPS 誘導(dǎo)的巨噬細(xì)胞炎癥反應(yīng)中，抑制含有炎性 miRNA-155 的外泌體的產(chǎn)生。

生物活性

Dexamethasone (Hexadecadrol) 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.

IC₅₀ & Target

Glucocorticoid receptor^[1]

體外研究(In Vitro)

Dexamethasone (Hexadecadrol) regulates several transcription factors, including activator protein-1, nuclear factor-AT, and nuclear factor-kB, leading to the activation and repression of key genes involved in the inflammatory response^[1].
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^[2].

體內(nèi)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)^[3].
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^[4].

分子量：392.46

Formula：C₂₂H₂₉FO₅

CAS 號：

50-02-2

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, protect from light

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

溶解性數(shù)據(jù)

In Vitro:

DMSO : 250 mg/mL (637.01 mM; ultrasonic and warming and heat to 60°C)

Ethanol : 8.33 mg/mL (21.23 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.5480 mL	12.7402 mL	25.4803 mL
5 mM	0.5096 mL	2.5480 mL	5.0961 mL
10 mM	0.2548 mL	1.2740 mL	2.5480 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 0.5% CMC-Na/saline water
Solubility: 18.18 mg/mL (46.32 mM); Suspended solution; Need ultrasonic
2.

請依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
4.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
5.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution

參考文獻(xiàn)

[1]. LaLone CA, et al. Effects of a glucocorticoid receptor agonist, Dexamethasone, on fathead minnow reproduction, growth, and development. Environ Toxicol Chem. 2012 Mar;31(3):611-22.

[2]. Adcock IM, et al. Ligand-induced differentiation of glucocorticoid receptor (GR) trans-repression and transactivation: preferential targetting of NF-kappaB and lack of I-kappaB involvement. Br J Pharmacol. 1999 Jun;127(4):1003-11

[3]. 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

[4]. Roussel D, et al. Dexamethasone treatment specifically increases the basal proton conductance of rat liver mitochondria. FEBS Lett. 2003 Apr 24;541(1-3):75-9.

[5]. Ballabh P, et al. Neutrophil and monocyte adhesion molecules in bronchopulmonary dysplasia, and effects of corticosteroids. Arch Dis Child Fetal Neonatal Ed. 2004 Jan;89(1):F76-83.

[6]. Heidi Ledford. et al. Coronavirus Breakthrough: Dexamethasone Is First Drug Shown to Save Lives. Nature. 2020 Jun 16.

[7]. Yun Chen, et al. Glucocorticoids inhibit production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses. Int J Clin Exp Pathol 2018;11(7):3391-3397.

Dexamethasone

Dexamethasone (Hexadecadrol) 是一種糖皮質(zhì)ji素受體 (glucocorticoid receptor) 激動劑。Dexamethasone 還顯著降低中性粒細(xì)胞的 CD11b，CD18 和 CD62L 表達(dá)，以及單核細(xì)胞的 CD11b 和 CD18 表達(dá)。Dexamethasone 有潛力用于 COVID-19 的研究。Dexamethasone 在 LPS 誘導(dǎo)的巨噬細(xì)胞炎癥反應(yīng)中，抑制含有炎性 miRNA-155 的外泌體的產(chǎn)生。

貨號：HY-14648
CAS：50-02-2

品牌：MCE

型號：HY-14648

起訂量：1

規(guī)格:：500mg

價格:：￥500

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在線客服

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產(chǎn)品詳情

Dexamethasone

Dexamethasone (Hexadecadrol) 是一種糖皮質(zhì)ji素受體 (glucocorticoid receptor) 激動劑。Dexamethasone 還顯著降低中性粒細(xì)胞的 CD11b，CD18 和 CD62L 表達(dá)，以及單核細(xì)胞的 CD11b 和 CD18 表達(dá)。Dexamethasone 有潛力用于 COVID-19 的研究。Dexamethasone 在 LPS 誘導(dǎo)的巨噬細(xì)胞炎癥反應(yīng)中，抑制含有炎性 miRNA-155 的外泌體的產(chǎn)生。

生物活性

Dexamethasone (Hexadecadrol) 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.

IC₅₀ & Target

Glucocorticoid receptor^[1]

體外研究(In Vitro)

Dexamethasone (Hexadecadrol) regulates several transcription factors, including activator protein-1, nuclear factor-AT, and nuclear factor-kB, leading to the activation and repression of key genes involved in the inflammatory response^[1].
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^[2].

體內(nèi)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)^[3].
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^[4].

分子量：392.46

Formula：C₂₂H₂₉FO₅

CAS 號：

50-02-2

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, protect from light

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

溶解性數(shù)據(jù)

In Vitro:

DMSO : 250 mg/mL (637.01 mM; ultrasonic and warming and heat to 60°C)

Ethanol : 8.33 mg/mL (21.23 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.5480 mL	12.7402 mL	25.4803 mL
5 mM	0.5096 mL	2.5480 mL	5.0961 mL
10 mM	0.2548 mL	1.2740 mL	2.5480 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 0.5% CMC-Na/saline water
Solubility: 18.18 mg/mL (46.32 mM); Suspended solution; Need ultrasonic
2.

請依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
4.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
5.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution