Beclomethasone 17-propionate
(Synonyms: 9Α-氯-16Β-甲基孕甾-1,4-二烯-11Β,17Α,21-三醇-3,20-二酮-17-丙酸酯,Beclomethasone-17-monopropionate; 17-BMP) 目录号 : GC61536
Beclomethasone17-propionate(Beclomethasone-17-monopropionate)是Beclomethasonedipropionate的活性代谢产物，是糖皮质激素受体(GR)激动剂。Beclomethasone17-propionate对GR的亲和力比Beclomethasonedipropionate高。Beclomethasone17-propionate有效抑制慢性阻塞性肺疾病(COPD)肺巨噬细胞中细胞因子的产生。
Cas No.:5534-18-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate , is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages[1][2][3].
Metabolism of Beclomethasone dipropionate to 17-BMP is an important activation step. Beclomethasone 17-propionate inhibits LPS-stimulated CXCL8, TNFα and IL-6. The EC50 values of Beclomethasone 17-propionate for IL-6, TNFα and CXCL8 were 0.05 nM, 0.01 nM and 0.1 nM, respectively. Beclomethasone 17-propionate evokes upregulation of the GR dependent genes FKBP51 and GILZ[3].
[1]. WÜrthwein G, et al. Activation of beclomethasone dipropionate by hydrolysis to beclomethasone-17-monopropionate. Biopharm Drug Dispos. 1990 Jul;11(5):381-94. [2]. Roberts JK, et al. Metabolism of beclomethasone dipropionate by cytochrome P450 3A enzymes. J Pharmacol Exp Ther. 2013 May;345(2):308-16. [3]. Plumb J, et al. Evaluation of glucocorticoid receptor function in COPD lung macrophages using beclomethasone-17-monopropionate. PLoS One. 2013 May 21;8(5):e64257.
| Cas No. | 5534-18-9 | SDF | |
| 别名 | 9Α-氯-16Β-甲基孕甾-1,4-二烯-11Β,17Α,21-三醇-3,20-二酮-17-丙酸酯,Beclomethasone-17-monopropionate; 17-BMP | ||
| Canonical SMILES | C[C@@]12[C@](C(CO)=O)(OC(CC)=O)[C@@H](C)C[C@@]1([H])[C@]3([H])CCC4=CC(C=C[C@]4(C)[C@@]3(Cl)[C@@H](O)C2)=O | ||
| 分子式 | C25H33ClO6 | 分子量 | 464.98 |
| 溶解度 | DMSO: 100 mg/mL (215.06 mM) | 储存条件 | -20°C, stored under nitrogen |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1506 mL | 10.7532 mL | 21.5063 mL |
| 5 mM | 0.4301 mL | 2.1506 mL | 4.3013 mL |
| 10 mM | 0.2151 mL | 1.0753 mL | 2.1506 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Does Vitamin D Work Synergistically with Anti-Asthmatic Drugs in Airway Remodeling?
Int J Mol Sci 2022 Oct 24;23(21):12798.PMID:36361588DOI:10.3390/ijms232112798.
Vitamin D is commonly known for its properties of airway remodeling inhibition. Due to this, we decided to analyze the action of calcitriol with anti-asthmatic drugs in airway remodeling. The HFL1 cell line was treated with calcitriol, Beclomethasone 17-propionate, montelukast sodium, LTD4 and TGF-β in different combinations. Real-time PCR was used to analyzed the expression of ACTA2, CDH-1, Vimentin, ADAM33, MMP-9 and CysLTR1 on the mRNA level, whereas Western blot was used to analyze gene expression on the protein level. One-way analysis variants, the Kruskal-Wallis test, Student's t-test or Welch's t-test were used for statistical analysis. Concerning the results, pre-treatment with calcitriol increased the inhibitory effect of Beclomethasone 17-propionate and montelukast sodium on the expression of ACTA2 (p = 0.0072), Vimentin (p = 0.0002) and CysLTR1 (p = 0.0204), and 1,25(OH)2D3 had an influence on the effects of Beclomethasone 17-propionate and montelukast sodium and of CDH1 expression (p = 0.0076). On the protein level, pre-treatment with calcitriol with Beclomethasone 17-propionate and montelukast sodium treatment decreased ACTA2 expression in comparison to the LT (LTD4 and TGF-β) control group (p = 0.0191). Hence, our study not only confirms that vitamin D may inhibit airway remodeling, but also shows that vitamin D has a synergistic effect with anti-asthmatic drugs.