| 产品介绍 |
Mupirocin (BRL-4910A, Pseudomonic acid) calcium hydrate 可从 Pseudomonas fluorescens 中分离得到,是一种有口服活性的抗生素。Mupirocin calcium hydrate 通过可逆地抑制异亮氨酸转移 RNA,从而抑制细菌蛋白和 RNA 的合成而发挥抗菌作用。
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| 生物活性 |
Mupirocin (BRL-4910A, Pseudomonic acid) calcium hydrate is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin calcium hydrate apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.
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| 体外研究 |
Mupirocin (BRL-4910A, Pseudomonic acid) calcium hydrate (0-100 μM; 48 h) shows antibacterial effect against staphylococci, streptococci and certain gram-negative bacteria, with MIC values range from 0.06-0.25 μg/mL (MIC50 =0.12 μg/mL, MIC90 =0.25 μg/mL).
Mupirocin calcium hydrate is highly bound (95% bound) to human serum protein, thus results in activity inhibition in the presence of human serum.
Mupirocin calcium hydrate apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.
Mupirocin calcium hydrate (2% ointment) reduces pro-inflammatory cytokines IL-1β and IL-17 level, decreases tumor necrosis factor-alpha (TNF-α) expression, and increases the leavel of vascular endothelial growth factor (VEGF)[4].
Mupirocin calcium hydrate inhibits MS (S. epidermidis ATCC 12228), MR (S. epidermidis (Se56-99)), and VIR (S. epidermidis (Se43-98)) with MICs of 0.25, 1.26, 1.59 mg/L[5].
Note: MIC, the minimum inhibition concentration.
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay
| Cell Line: |
Staphylococcus aureus |
| Concentration: |
0-100 μM/mL |
| Incubation Time: |
24, 48 hours |
| Result: |
Resulted in a 90 to 99% reduction at 24 h, with MIC values ranged from 0.12-1.0 μM/mL and MBC values ranged from 4.0-32 μM/mL at 48 h.
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体内研究 (In Vivo) |
MRSA: Meticillin-resistant Staphylococcus aureus
Mupirocin (BRL-4910A, Pseudomonic acid) calcium is well absorbed after oral and parenteral administration but serum antibiotic concentrations were short-lived as a result of extensive degradation to the antibacterially inactive metabolite, monic acid A.
Mupirocin calcium (2% ointment; external administration; twice daily; 3-6 d) decreases the total bacterial loads in the skin lesions with either topical treatment.
Mupirocin calcium (2% ointment; external administration; 4 d) alleviates MRSA-infected pressure ulcers in mice[4].
Mupirocin calcium (100 mg/mL; s.c.; 7 d) exerts prevention efficacy against vascular prosthetic graft infection due to Staphylococcus epidermidis[5].
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
MRSA skin infection model in mice (10-12 weeks old) |
| Dosage: |
2% ointment |
| Administration: |
External administration; twice daily; 3-6 days |
| Result: |
Reduced the total bacterial loads in the skin lesions, and decreased by 2.0, 5.1 log10 CFU on day 3 and 6, respectively.
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| Animal Model: |
Diabetic pressure ulcer mouse model (33.2-39.2 g)[4] |
| Dosage: |
2% ointment |
| Administration: |
External administration; 4 days |
| Result: |
Resulted less superficial mats of bacterial colonies, and improved histopathology evaluation.
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| Animal Model: |
Adult male Wistar rats (weight 275-325 g)[5] |
| Dosage: |
Impregnated with 100 μg of mupirocin/mL; segments:1.5 cm *1 cm2
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| Administration: |
Subcutaneous implantation; 7 days |
| Result: |
Resulted in preventing S. epidermidis infection of the graft in a rat model with spontaneously bound to collagen-sealed Dacron grafts.
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| 体内研究 |
MRSA: Meticillin-resistant Staphylococcus aureus
Mupirocin (BRL-4910A, Pseudomonic acid) calcium is well absorbed after oral and parenteral administration but serum antibiotic concentrations were short-lived as a result of extensive degradation to the antibacterially inactive metabolite, monic acid A.
Mupirocin calcium (2% ointment; external administration; twice daily; 3-6 d) decreases the total bacterial loads in the skin lesions with either topical treatment.
Mupirocin calcium (2% ointment; external administration; 4 d) alleviates MRSA-infected pressure ulcers in mice[4].
Mupirocin calcium (100 mg/mL; s.c.; 7 d) exerts prevention efficacy against vascular prosthetic graft infection due to Staphylococcus epidermidis[5].
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
MRSA skin infection model in mice (10-12 weeks old) |
| Dosage: |
2% ointment |
| Administration: |
External administration; twice daily; 3-6 days |
| Result: |
Reduced the total bacterial loads in the skin lesions, and decreased by 2.0, 5.1 log10 CFU on day 3 and 6, respectively.
|
| Animal Model: |
Diabetic pressure ulcer mouse model (33.2-39.2 g)[4] |
| Dosage: |
2% ointment |
| Administration: |
External administration; 4 days |
| Result: |
Resulted less superficial mats of bacterial colonies, and improved histopathology evaluation.
|
| Animal Model: |
Adult male Wistar rats (weight 275-325 g)[5] |
| Dosage: |
Impregnated with 100 μg of mupirocin/mL; segments:1.5 cm *1 cm2
|
| Administration: |
Subcutaneous implantation; 7 days |
| Result: |
Resulted in preventing S. epidermidis infection of the graft in a rat model with spontaneously bound to collagen-sealed Dacron grafts.
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| 体内研究 |
MRSA: Meticillin-resistant Staphylococcus aureus
Mupirocin (BRL-4910A, Pseudomonic acid) calcium is well absorbed after oral and parenteral administration but serum antibiotic concentrations were short-lived as a result of extensive degradation to the antibacterially inactive metabolite, monic acid A.
Mupirocin calcium (2% ointment; external administration; twice daily; 3-6 d) decreases the total bacterial loads in the skin lesions with either topical treatment.
Mupirocin calcium (2% ointment; external administration; 4 d) alleviates MRSA-infected pressure ulcers in mice[4].
Mupirocin calcium (100 mg/mL; s.c.; 7 d) exerts prevention efficacy against vascular prosthetic graft infection due to Staphylococcus epidermidis[5].
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
MRSA skin infection model in mice (10-12 weeks old) |
| Dosage: |
2% ointment |
| Administration: |
External administration; twice daily; 3-6 days |
| Result: |
Reduced the total bacterial loads in the skin lesions, and decreased by 2.0, 5.1 log10 CFU on day 3 and 6, respectively.
|
| Animal Model: |
Diabetic pressure ulcer mouse model (33.2-39.2 g)[4] |
| Dosage: |
2% ointment |
| Administration: |
External administration; 4 days |
| Result: |
Resulted less superficial mats of bacterial colonies, and improved histopathology evaluation.
|
| Animal Model: |
Adult male Wistar rats (weight 275-325 g)[5] |
| Dosage: |
Impregnated with 100 μg of mupirocin/mL; segments:1.5 cm *1 cm2
|
| Administration: |
Subcutaneous implantation; 7 days |
| Result: |
Resulted in preventing S. epidermidis infection of the graft in a rat model with spontaneously bound to collagen-sealed Dacron grafts.
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| 性状 | Solid |
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| 溶解性数据 |
In Vitro:
DMSO : 100 mg/mL (185.64 mM; Need ultrasonic)
配制储备液
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浓度
溶剂体积
质量
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1 mg |
5 mg |
10 mg |
| 1 mM |
1.8564 mL |
9.2819 mL |
18.5639 mL |
| 5 mM |
0.3713 mL |
1.8564 mL |
3.7128 mL |
| 10 mM |
0.1856 mL |
0.9282 mL |
1.8564 mL |
*
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制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
-
1.
请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% saline Solubility: ≥ 1.25 mg/mL (2.32 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (2.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。
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2.
请依序添加每种溶剂: 10% DMSO 90% (20% SBE-β-CD in saline) Solubility: ≥ 1.25 mg/mL (2.32 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (2.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。
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3.
请依序添加每种溶剂: 10% DMSO 90% corn oil Solubility: ≥ 1.25 mg/mL (2.32 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (2.32 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。
*以上所有助溶剂都可在 西域 网站选购。
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
4°C, sealed storage, away from moisture and light
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| 参考文献 |
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. Sutherland R, et al. Antibacterial activity of mupirocin (pseudomonic acid), a new antibiotic for topical use. Antimicrob Agents Chemother. 1985 Apr;27(4):495-8.
[Content Brief]
. Parenti MA, et al. Mupirocin: a topical antibiotic with a unique structure and mechanism of action. Clin Pharm. 1987 Oct;6(10):761-70.
[Content Brief]
. Vingsbo Lundberg C, et al. Efficacy of topical and systemic antibiotic treatment of meticillin-resistant Staphylococcus aureus in a murine superficial skin wound infection model. Int J Antimicrob Agents. 2013 Sep. 42(3):272-5.
[Content Brief]
[4]. Mohammad H, Abutaleb NS, Dieterly AM, Lyle LT, Seleem MN. Investigating auranofin for the treatment of infected diabetic pressure ulcers in mice and dermal toxicity in pigs. Sci Rep. 2021 May 25;11(1):10935.
[Content Brief]
[5]. Giacometti A, et al. Mupirocin prophylaxis against methicillin-susceptible, methicillin-resistant, or vancomycin-intermediate Staphylococcus epidermidis vascular-graft infection. Antimicrob Agents Chemother. 2000 Oct. 44(10):2842-4.
[Content Brief]
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