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/ Beclometasone Dipropionate/丙酸倍氯米松

Beclometasone Dipropionate/丙酸倍氯米松 {[allProObj[0].p_purity_real_show]}

货号：A739014 同义名： 二丙酸倍氯米松 / Beclomethasone dipropionate

Beclometasone Dipropionate是beclometasone的前药，是一种糖皮质激素激动剂，用于研究鼻炎和鼻窦炎。

Beclometasone Dipropionate/丙酸倍氯米松 化学结构 CAS号：5534-09-8
Beclometasone Dipropionate/丙酸倍氯米松 化学结构
CAS号：5534-09-8
Beclometasone Dipropionate/丙酸倍氯米松 3D分子结构
CAS号：5534-09-8
Beclometasone Dipropionate/丙酸倍氯米松 化学结构 CAS号：5534-09-8
Beclometasone Dipropionate/丙酸倍氯米松 3D分子结构 CAS号：5534-09-8
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Beclometasone Dipropionate/丙酸倍氯米松 纯度/质量文件 产品仅供科研

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Beclometasone Dipropionate/丙酸倍氯米松 生物活性

描述 Betamethasone dipropionate, the prodrug of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release. When mice were pretreated with betamethasone (5 mg/kg, po), MMP2 and MMP9 activities, TNF-alpha in BAL fluids, and the enhanced neutrophil number of LPS-exposed mice were reduced, whereas the level of IL-10 was increased[3]. Oral BDP (Beclometasone Dipropionate) gave an overall treatment result in patients with active ulcerative colitis without signs of systemic side-effects[4]. Sustained clinical and histological remission was induced with the topical steroid preparation, beclometasone dipropionate (Clipper), with no adverse effects[5]. Beclometasone dipropionate (BDP) is a topically active corticosteroid with low absorption into the systemic circulation, which minimises many of the deleterious side effects associated with systemic corticosteroids[6].

Beclometasone Dipropionate/丙酸倍氯米松 细胞实验

Cell Line
Concentration Treated Time Description References
BEAS2B bronchial epithelial cells 0.1-1,000 nM 24 h To assess the effects of BDP on bacterial burden and the antimicrobial peptide hCAP-18/LL-37, results showed BDP only increased bacterial loads and suppressed hCAP-18/LL-37 induction at the highest concentration (1,000 nM). Chest. 2020 Sep;158(3):947-951.
BEAS2B bronchial epithelial cells 0.1-1,000 nM 1 hour To evaluate the anti-inflammatory effects of BDP during bacterial infection, results showed BDP significantly suppressed induction of IL-6 and CXCL8/IL-8 at 10 nM or higher concentrations, but the effects were weaker than FP and budesonide. Chest. 2020 Sep;158(3):947-951.
fast-twitch fibre bundles 250 nM 10 min To investigate the rapid/non-genomic effects of BDP on maximum isometric force in fast-twitch muscle fibre bundles, results showed that 250 nM BDP did not significantly affect maximum isometric force. J Physiol. 2013 Oct 15;591(20):5171-85.
slow-twitch fibre bundles 250 nM 10 min To investigate the rapid/non-genomic effects of BDP on maximum isometric force in slow-twitch muscle fibre bundles, results showed that 250 nM BDP significantly increased maximum isometric force within 10 min. J Physiol. 2013 Oct 15;591(20):5171-85.
Hep-2 cells 1 and 5 μM 72 h Evaluate the effect of Beclomethasone on Chlamydophila pneumoniae infection. Results showed that Beclomethasone significantly reduced the number of infected cells at concentrations of 1 and 5 μM. Antimicrob Agents Chemother. 2004 Dec;48(12):4878-81

Beclometasone Dipropionate/丙酸倍氯米松 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice Chlamydophila pneumoniae infection model Subcutaneous injection 120 μg/kg/day Once a day for 4 consecutive days Evaluate the therapeutic effect of Beclomethasone combined with antibiotics on Chlamydophila pneumoniae infection. Results showed that the combination treatment significantly reduced the number of infected cells. Antimicrob Agents Chemother. 2004 Dec;48(12):4878-81
C57BL/6 mice Streptococcus pneumoniae infection model Intranasal administration 20 µg Single dose To evaluate the effects of BDP on inflammation and antibacterial immunity in vivo, results showed FP and budesonide significantly suppressed IL-6, tumor necrosis factor, IL-1β, and CXCL2/MIP-2, and reduced neutrophil recruitment, while BDP had weaker effects. Additionally, FP and budesonide increased lung bacterial loads and suppressed induction of the antimicrobial peptide CRAMP, whereas BDP had no significant effects. Chest. 2020 Sep;158(3):947-951.

Beclometasone Dipropionate/丙酸倍氯米松 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00854360 Seasonal Allergic Rhinitis ... 展开 >> Hayfever 收起 << Phase 2 Completed - -
NCT00854360 - Completed - -
NCT01345916 Asthma Phase 3 Completed - Poland ... 展开 >> GSPZOZ Uniwersytecki Szpital Kliniczny Łódź, Poland, 90-153 收起 <<

Beclometasone Dipropionate/丙酸倍氯米松 参考文献

[1]Ratner PH, Melchior A, et al. Pharmacokinetic profile of beclomethasone dipropionate hydrofluoroalkane after intranasal administration versus oral inhalation in healthy subjects: results of a single-dose, randomized, open-label, 3-period crossover study. Clin Ther. 2012 Jun;34(6):1422-31.

[2]Busse WW, Brazinsky S, et al. Efficacy response of inhaled beclomethasone dipropionate in asthma is proportional to dose and is improved by formulation with a new propellant. J Allergy Clin Immunol. 1999 Dec;104(6):1215-22.

[3]Corbel M, Lagente V, Théret N, Germain N, Clément B, Boichot E. Comparative effects of betamethasone, cyclosporin and nedocromil sodium in acute pulmonary inflammation and metalloproteinase activities in bronchoalveolar lavage fluid from mice exposed to lipopolysaccharide. Pulm Pharmacol Ther. 1999;12(3):165-71

[4]Campieri M, Adamo S, Valpiani D, D'Arienzo A, D'Albasio G, Pitzalis M, Cesari P, Casetti T, Castiglione GN, Rizzello F, Manguso F, Varoli G, Gionchetti P. Oral beclometasone dipropionate in the treatment of extensive and left-sided active ulcerative colitis: a multicentre randomised study. Aliment Pharmacol Ther. 2003 Jun 15;17(12):1471-80

[5]Ibraheim H, Green M, Papa S, Powell N. Topical beclometasone dipropionate in the management of immune checkpoint inhibitor-induced microscopic colitis. BMJ Case Rep. 2019 Apr 3;12(4):e226481

[6]Díez-Campelo M, Sánchez-Guijo FM, Pérez-Simón JA. Beclometasone dipropionate: a topically active corticosteroid for the treatment of gastrointestinal graft-versus-host disease. Expert Opin Investig Drugs. 2008 Sep;17(9):1389-401

Beclometasone Dipropionate/丙酸倍氯米松 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.60mL

1.92mL

0.96mL

19.19mL

3.84mL

1.92mL

Beclometasone Dipropionate/丙酸倍氯米松 技术信息

CAS号5534-09-8
分子式C28H37ClO7
分子量 521.04
SMILES Code CCC(O[C@]1(C(COC(CC)=O)=O)[C@@H](C)C[C@@]2([H])[C@]3([H])CCC4=CC(C=C[C@]4(C)C3(Cl)[C@@H](O)C[C@]12C)=O)=O
MDL No. MFCD00135613
别名 二丙酸倍氯米松 ;Beclomethasone dipropionate
运输蓝冰
InChI Key KUVIULQEHSCUHY-XYWKZLDCSA-N
Pubchem ID 21700
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

DMSO: 105 mg/mL(201.52 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二

Tags: Beclometasone | 5534-09-8 | Beclomethasone dipropionate | Glucocorticoid Receptor | Glucocorticoid Receptor Agonist | Immunology/Inflammation | Vitamin D Related/Nuclear Receptor | NF-κB | Metabolic Enzyme/Protease | Glucocorticoid Receptor | Reactive Oxygen Species | NO Synthase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Beclometasone Dipropionate/丙酸倍氯米松 纯度/质量文件 | Beclometasone Dipropionate/丙酸倍氯米松 生物活性 | Beclometasone Dipropionate/丙酸倍氯米松 临床数据 | Beclometasone Dipropionate/丙酸倍氯米松 参考文献 | Beclometasone Dipropionate/丙酸倍氯米松 实验方案 | Beclometasone Dipropionate/丙酸倍氯米松 技术信息

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