Beclometasone (Beclomethasone)
(Synonyms: 倍氯米松; Beclomethasone) 目录号 : GC33856
A glucocorticoid
Cas No.:4419-39-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | The transgenic lines Tg(fli1:GFP) and Tg(mpx:GFP) are used in this study. 0.2 mM N-phenylthiourea (PTU) is applied to prevent pigment formation from 1 day post-fertilization (dpf). For Pu.1 knockdown, Pu.1 MO (1 mM for partial knockdown and 2 mM for complete knockdown is injected into the yolk at the one-cell stage. For pharmacological inhibition, the VEGFR tyrosine kinase inhibitors KRN633 (0.1-1 μM) or Sunitinib (0.1-1 μM), Beclomethasone (25 μM) and β-amino-proprionitrile (βAPN, 500 μM) are applied directly to the egg water and refreshed every 2 days. For pharmacological inhibition, Beclomethasone is applied to the embryos 4 h before implantation and KRN633, Sunitinib and βAPN are applied 4-6 h post-implantation. For each cell line or condition, data are representative of ≥ three independent experiments, with ≥30 embryos/group. Experiments are discarded when the survival rate of the control group is <90%[1]. |
References: [1]. He S, et al. Neutrophil-mediated experimental metastasis is enhanced by VEGFR inhibition in a zebrafish xenograft model. J Pathol. 2012 Aug;227(4):431-45. | |
Beclomethasone is a glucocorticoid.1 It reduces plasma corticosteroid levels in rats when administered at doses ranging from 1 to 10 mg/kg.
1.Yamamoto, S.Glucocorticoid action of beclomethasone and its propionate ester derivativesNihon Yakurigaku Zasshi73(1)25-36(1976)
| Cas No. | 4419-39-0 | SDF | |
| 别名 | 倍氯米松; Beclomethasone | ||
| Canonical SMILES | C[C@@]12[C@](C(CO)=O)(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 | C22H29ClO5 | 分子量 | 408.92 |
| 溶解度 | DMSO : ≥ 32 mg/mL (78.25 mM) | 储存条件 | Store at -20°C |
| 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 | 2.4455 mL | 12.2273 mL | 24.4547 mL |
| 5 mM | 0.4891 mL | 2.4455 mL | 4.8909 mL |
| 10 mM | 0.2445 mL | 1.2227 mL | 2.4455 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。
Beclomethasone dipropionate
Ann Intern Med 1981 Oct;95(4):464-7.PMID:6792963DOI:10.7326/0003-4819-95-4-464.
Experience with Beclomethasone dipropionate during the past 5 years has confirmed and extended the original observation that it is an effective, topically active corticosteroid of great value in treating asthma. Most steroid-dependent asthmatic patients can be successfully controlled with the drug, at least most of the time, and the therapeutic effect is dose dependent. Although high doses may be associated with some adrenal suppression such doses do not cause systemic symptoms, and side effects are of little consequence. It is important that patients treated with steroid aerosols continue to receive other effective therapeutic agents, notably adrenergic drugs, particularly by aerosol, and theophylline compounds; that they learn how to inhale the aerosol properly; and, most important, that they promptly start taking oral steroids when they experience an exacerbation of asthma.
Inhaled Beclometasone dipropionate/formoterol fumarate extrafine fixed combination for the treatment of asthma
Expert Rev Respir Med 2016;10(5):481-90.PMID:26938578DOI:10.1586/17476348.2016.1161508.
Inhaled therapy is often considered the cornerstone of asthma management and international guidelines recommend combination therapy of inhaled corticosteroids (ICS) and long-acting-beta2-agonists (LABA) in a large proportion of asthmatic patients. The effectiveness of ICS/LABA is dependent on the correct choice of device and proper inhalation technique, this influences drug delivery and distribution along the bronchial tree, including the most peripheral airways. The fixed combination of Beclometasone dipropionate/formoterol fumarate (BDP/FF) is the only extrafine formulation available in pressurized metered dose inhaler (pMDI) and in dry powder inhaler (DPI). Here, we focus on the recent significant advances regarding BDP/FF fixed combination for the treatment of asthma.
High-dose Beclometasone dipropionate/formoterol fumarate in fixed-dose combination for the treatment of asthma
Ther Adv Respir Dis 2016 Oct;10(5):492-502.PMID:27340255DOI:10.1177/1753465816654442.
The high-strength formulation of extrafine Beclometasone dipropionate/formoterol fumarate (BDP/Form) 200/6 µg has been developed to step up inhaled corticosteroid treatment, without increasing the dose of the bronchodilator, in patients who are not controlled with previous therapies. Two clinical studies have evaluated efficacy of high-strength BDP/Form as compared with another high-dose fixed combination and BDP monotherapy. Overall, data show that BDP/Form 200/6 μg improves lung function and has beneficial effects on symptoms, use of rescue medication and asthma control, with an acceptable safety profile comparable with that of high-dose fluticasone propionate/salmeterol. Therefore, BDP/Form 200/6 μg could be considered as an effective and safe treatment for patients with asthma who are not adequately controlled with high doses of inhaled corticosteroid monotherapy or medium doses of inhaled corticosteroid/long-acting β2-agonist combinations.
Beclometasone oral--DOR BioPharma
Drugs R D 2007;8(2):91-4.PMID:17324006DOI:10.2165/00126839-200708020-00003.
orBec is an oral enteric-coated tablet formulation of the corticosteroid Beclometasone, which has been developed by Enteron Pharmaceuticals, a subsidiary of Corporate Technology Development (now DOR BioPharma). orBec is being developed for the treatment of gastrointestinal graft-versus-host disease (GVHD) and an NDA has been filed in the US. DOR BioPharma has also filed an MAA in Europe for the same indication.orBec is designed to reduce the need for systemic immunosuppressive drugs, thereby improving the outcome of bone marrow and stem cell transplantation.DOR BioPharma may seek a marketing partner in the US and elsewhere for orBec in GVHD and will seek a partner for other potential indications of the drug.In December 2001, Corporate Technology Development was acquired by Endorex Corporation (now DOR BioPharma). In October 1998, Enteron Pharmaceuticals (DOR BioPharma) entered into an exclusive, worldwide, royalty bearing license agreement with George B. McDonald, MD, including the right to grant sublicenses, for the rights to the intellectual property and know-how relating to orBec. In January 2007, DOR BioPharma received $US3 million under a non-binding letter of intent from Sigma-Tau Pharmaceuticals. The agreement grants Sigma-Tau an exclusive right to negotiate terms and conditions for a possible business transaction or strategic alliance regarding orBec and potentially other DOR pipeline compounds until 1 March 2007. Under the terms of the agreement, Sigma-Tau purchased $US1 million of DOR's common stock, with an additional $US2 million paid in cash. If no agreement is reached by 1 March 2007, DOR will return the $US2 million to Sigma-Tau within 60 days. DOR BioPharma received an unsolicited proposal from Cell Therapeutics, Inc. to acquire DOR BioPharma in January 2007. Because of the non-binding agreement already signed with Sigma-Tau, DOR BioPharma's board of directors cannot consider Cell Therapeutics' merger proposal at this time. orBec has been filed for approval in the US for the treatment of gastrointestinal GVHD. The US FDA accepted the NDA filing and has established a target date of 21 July 2007 for completion of review of the NDA. In November 2006, the EMEA determined that the MAA for orBec for the treatment of gastrointestinal GVHD is complete and that the review process has begun. The data provided in the MAA and NDA submissions demonstrate that orBec safely provides a lower risk of mortality compared with the current standard of care. Both filings are supported by data from two randomised, double-blinded, placebo-controlled clinical trials. The first was a 129-patient pivotal phase III clinical trial for orBec conducted at 16 bone marrow/stem cell transplant centres in the US and France. The second trial was a 60-patient phase II clinical trial conducted at the Fred Hutchinson Cancer Research Centre. In the primary endpoint of its pivotal trial, time to treatment failure through day 50, orBec failed to achieve statistical significance (p-value 0.1177). However, orBec did achieve statistical significance in the secondary endpoints of time to treatment failure through day 80, and a reduction in mortality compared with placebo. In this trial, patient survival at the prespecified endpoint of 200 days post-transplant showed a statistically significant 66% reduction in mortality among patients randomised to orBec. DOR BioPharma believes the primary endpoint was not achieved due to a higher than expected rate of treatment failures during the initial 10 days in both treatment groups. The mortality benefit in favour of orBec was confirmed in a retrospective analysis of the phase II study, in which there was a 55% reduction in mortality at 200 days post-transplant. At 1 year after randomisation, there were relatively consistent 51% and 45% reductions in the risk of mortality among patients randomised to orBec in both the phase III and phase II studies, respectively.DOR BioPharma is also conducting a phase II clinical trial to investigate orBec in the prevention of gastrointestinal GVHD. DOR BioPharma has executed an exclusive licence agreement with the University of Texas Medical Branch at Galveston for the use of oral luminally active anti-inflammatory drugs, such as orBec, for the treatment of irritable bowel syndrome.
Practical and scalable synthesis of Beclomethasone dipropionate
Steroids 2022 Jan;177:108948.PMID:34871605DOI:10.1016/j.steroids.2021.108948.
Beclomethasone dipropionate (1) is a synthetic corticosteroid with anti-inflammatory, antipruritic, and anti-allergy properties. It is widely used to treat asthma, allergic rhinitis, and dermatoses. However, existing synthetic routes to this active pharmaceutical ingredient (API) contain steps resulting in low and/or inconsistent yields, and use obsolete reagents. Such inconsistencies coupled with a lack of reliable experimental data makes laboratory-scale and large-scale synthesis of this API difficult and time-consuming. In this paper, we report a practical and scalable approach to synthesize 1 from the readily available steroidal intermediate, 16β-methyl epoxide (3, DB-11). A gram-scale to kilogram-scale synthesis of 1 was achieved with 82% yield, using a cost-effective and scalable methodology. Selective propionylation of the hydroxyl groups at C17 and C21 demonstrate the fact that this approach can be conveniently implemented in fine chemical industries.