Mometasone
(Synonyms: 莫米松-d3EP杂质G)) 目录号 : GC47698
A synthetic glucocorticoid with anti-inflammatory and anti-allergic activities
Cas No.:105102-22-5
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
Mometasone is a synthetic glucocorticoid with anti-inflammatory and anti-allergic activities.1,2,3 In vivo, mometasone (3 mg/kg) reduces pulmonary edema and neutrophil infiltration in a mouse model of chlorine-induced chemical lung injury.1 Intranasal administration of mometasone (0.2 µg/animal) reduces nose-rubbing behavior, sneezing, and nasal mucosal levels of IL-4 in a mouse model of allergic rhinitis.2 Mometasone also reduces nasal mucosal epithelial destruction, fibrosis, and cilia loss in a rat model of rhinitis medicamentosa induced by oxymetazoline .
1.Kitlevsen, D.K., Povlsen, G.K., Berezin, V., et al.NCAM-induced intracellular signaling revisitedJ. Neurosci. Res.86(4)727-743(2008) 2.Williams, E.J., Furness, J., Walsh, F.S., et al.Activation of the FGF receptor underlies neurite outgrowth stimulated by L1, N-CAM, and N-cadherinNeuron.13(3)583-594(1994) 3.Van Acker, H.H., Van Acker, Z.P., Versteven, M., et al.CD56 homodimerization and participation in anti-tumor immune effector cell functioning: A role for interleukin-15Cancers (Basel)11(7)1029(2019)
| Cas No. | 105102-22-5 | SDF | |
| 别名 | 莫米松-d3EP杂质G) | ||
| Canonical SMILES | Cl[C@@]12[C@](CCC([C@@]2(C=C3)C)=CC3=O)([H])[C@@]4([H])[C@](C[C@@H]1O)([C@](C(CCl)=O)(O)[C@@H](C4)C)C | ||
| 分子式 | C22H28Cl2O4 | 分子量 | 427.4 |
| 溶解度 | Methanol: Slightly soluble | 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 | 2.3397 mL | 11.6986 mL | 23.3973 mL |
| 5 mM | 0.4679 mL | 2.3397 mL | 4.6795 mL |
| 10 mM | 0.234 mL | 1.1699 mL | 2.3397 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。
Comparative safety and efficacy of topical Mometasone furoate with other topical corticosteroids
Australas J Dermatol 2018 Aug;59(3):e168-e174.PMID:29411351DOI:10.1111/ajd.12762.
Derivatives of hydrocortisone, such as Mometasone furoate, a (2') furoate-17 ester with chlorine substitutions at positions 9 and 21, have been designed to improve efficacy and reduce the incidence of adverse effects. An extensive literature search of MEDLINE, Embase and other databases was conducted to review the safety and efficacy of various formulations of topical Mometasone furoate. Mometasone furoate exhibits high potency with greater anti-inflammatory activity and a longer duration of action than betamethasone. In clinical trials, Mometasone furoate shows comparable or significantly better efficacy, depending on the comparator, in all indications studied in both adults and children. It is well tolerated with only transient, mild to moderate local adverse effects. It is characterised by low systemic availability due to its high lipophilicity, low percutaneous absorption and rapid hepatic biotransformation, and consequently has no significant effect on the hypothalamic-pituitary-adrenal axis. The molecular biotransformation of Mometasone furoate in the skin results in a lower affinity with dermal cells than epidermal cells, which contributes to its low atrophogenicity. Sensitisation to Mometasone furoate is low. Overall, Mometasone furoate is a highly efficacious potent corticosteroid with a low risk of both local and systemic adverse effects.
Indacaterol/Glycopyrronium/Mometasone: A Review in Asthma
Drugs 2021 Apr;81(6):709-719.PMID:33871819DOI:10.1007/s40265-021-01518-w.
Indacaterol/glycopyrronium/Mometasone (Enerzair® Breezhaler®) is a fixed-dose combination of the long-acting β2 agonist (LABA) indacaterol, the long-acting muscarinic antagonist (LAMA) glycopyrronium and the inhaled corticosteroid (ICS) Mometasone furoate (hereafter referred to as Mometasone) delivered via a capsule-based dry-powder inhaler. It is approved in the EU for use as maintenance treatment in adult patients with inadequately controlled asthma who had experienced one or more exacerbations in the previous year. The approval also includes an optional digital companion (sensor and app) that provides data on the patient's use of the inhaler. In the 52-week IRIDIUM trial in patients with inadequately controlled asthma, indacaterol/glycopyrronium/Mometasone improved lung function to a greater extent than LABA/ICS combinations (i.e. indacaterol/Mometasone and fluticasone propionate/salmeterol), but superiority in Asthma Control Questionnaire 7 score was not shown. In the 24-week ARGON trial, indacaterol/glycopyrronium/Mometasone via a single inhaler was non-inferior to fluticasone propionate/salmeterol + tiotropium via two inhalers with regard to Asthma Quality of Life Questionnaire score. Indacaterol/glycopyrronium/Mometasone was generally well tolerated, and the most common adverse events were respiratory in nature. In conclusion, combination therapy with indacaterol/glycopyrronium/Mometasone represents a valuable option for the maintenance treatment of asthma, with the convenience of once-daily administration via a single inhaler.
Inhaled indacaterol/glycopyrronium/Mometasone furoate fixed-dose combination in moderate-to-severe asthma
Expert Rev Respir Med 2022 Jan;16(1):1-15.PMID:34783265DOI:10.1080/17476348.2021.2005585.
Introduction: Fixed-dose long-acting beta2-agonist (LABA)/inhaled corticosteroid (ICS) combinations and add-on therapies as needed are the mainstay for maintenance therapy in asthma. However, more than 40% of patients have an inadequately controlled disease. The development of triple fixed-dose combinations consisting of long-acting muscarinic antagonist (LAMA)/LABA/ICS has paved the way for a new approach to reach therapeutic goals of an optimal control of symptoms and an effective prevention of future exacerbations. Areas covered: A search was conducted on PubMed (MEDLINE), using the MeSH terms [asthma] + [indacaterol] + [glycopyrronium] +[Mometasone furoate] + [treatment], until October 2021. Original data from clinical trials, prospective and retrospective studies and reviews were selected. Clinical studies with IND/MF/GLY (Enerzair Breezhaler) are summarized, and its place in current asthma therapy is examined. Expert opinion: Triple therapy has been shown to be an effective and safe therapeutic option for asthma patients who remain uncontrolled despite ICS/LABA combination. The recently approved single-inhaler indacaterol/glycopyrronium/Mometasone fixed dose combination has demonstrated to significantly reduce exacerbations, improve FEV1, symptoms and quality of life compared to ICS/LABA, including, salmeterol/fluticasone combination. Moreover, once-daily dosing may improve adherence.
Mometasone furoate nasal spray in the treatment of patients with COVID-19 olfactory dysfunction: A randomized, double blind clinical trial
Int Immunopharmacol 2021 Sep;98:107871.PMID:34147912DOI:10.1016/j.intimp.2021.107871.
The aim of this study was to evaluate the usage of Mometasone furoate nasal spray in the recovery of patients with severe microsmia or anosmia induced by COVID-19. This was a prospective clinical trial on non-hospitalized adult patients with COVID-19 (>18 years) who had severe microsmia or anosmia within two weeks. The subjects were randomly assigned to the Mometasone furoate group (100 mcg twice daily) or sodium chloride group (0.9%); both groups also received olfactory training for 4 weeks. The primary outcome was the improvement of the olfactory score at the end of the study. Visual analog scale (VAS) and the University of Pennsylvania Smell Identification Test (UPSIT) were used to assess primary outcome. A total of 80 patients were recruited, 77 of them completed the study and were analyzed. There was no statistically significant difference in terms of demographics and baseline clinical characteristics. The olfactory scores (based on VAS) at weekly intervals showed a significant difference between the two groups (P:0.318, <0.001, <0.001, <0.001, respectively). The analyses also showed significant within-group differences from baseline. Nevertheless, the changes were not significant between the two groups (P: 0.444, 0.402, 0.267, 0.329). There was no significant difference between the two groups in terms of the UPSIT results (p > 0.239). However, a significant between-group difference was noted in the severity of loss of smell (P < 0.001). Compared to olfactory training, Mometasone furoate nasal spray combination with olfactory training showed a higher improvement in severe chronic anosmia by COVID-19.
Mometasone furoate nasal spray for the treatment of asthma
Expert Opin Investig Drugs 2016 Aug;25(8):999-1004.PMID:27218300DOI:10.1080/13543784.2016.1192124.
Introduction: Asthma is a common respiratory disease characterized by airway inflammation, bronchoconstriction and airway hyperresponsiveness and symptoms such as coughing, wheezing, shortness of breath and chest tightness. Allergic rhinitis is a common comorbidity in asthma and glucocorticoids are the key stone in the treatment of both diseases. Mometasone furoate is a potent synthetic steroid with a very high receptor affinity and a low bioavailability and shown to be superior compared to other inhaled corticosteroids. It is not clear whether the use of Mometasone furoate nasal spray (MFNS) is associated with an improvement in asthma control. Areas covered: This current paper reviews the current knowledge on the effect of Mometasone furoate nasal spray in the treatment of asthma and includes clinical trials in which both subjective and objective outcomes are assessed. Expert opinion: To date, only few clinical studies have investigated the effect of nasal steroids in the treatment of asthma. The studies investigating the effect of MFNS report contradicting results, although the most well-designed study to answer this question finds no improvement in asthma control. Thus, it seems unlikely that asthma guidelines will be influenced by the current knowledge on the effect of MFNS in the treatment of asthma.