Mupirocin calcium hydrate (Synonyms: BRL-4910A calcium hydrate; Pseudomonic acid calcium hydrate)

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Mupirocin calcium hydrate  (Synonyms: BRL-4910A calcium hydrate; Pseudomonic acid calcium hydrate) 纯度: 98.05%

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。

Mupirocin calcium hydrate (Synonyms: BRL-4910A calcium hydrate; Pseudomonic acid calcium hydrate)

Mupirocin calcium hydrate Chemical Structure

CAS No. : 115074-43-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥770 In-stock
25 mg ￥700 In-stock
50 mg ￥1200 In-stock
100 mg ￥1900 In-stock
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500 mg   询价  

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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[1][2].

体外研究
(In Vitro)

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)[1].
Mupirocin calcium hydrate is highly bound (95% bound) to human serum protein, thus results in activity inhibition in the presence of human serum[1].
Mupirocin calcium hydrate apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis[2].
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.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Mupirocin calcium hydrate 相关抗体:

Cell Viability Assay[1]

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.

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[1].
Mupirocin calcium (2% ointment; external administration; twice daily; 3-6 d) decreases the total bacterial loads in the skin lesions with either topical treatment[3].
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].

Shanghai Jinpan Biotech Co Ltd 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)[3]
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.

Clinical Trial

分子量

538.68

Formula

C26H46O10
CAS 号

115074-43-6
性状

固体

颜色

White to off-white

结构分类
  • Antibiotics
  • Disease Research
  • Antibacterial
  • Antibiotics
  • Other Antibiotics
初始来源
  • 微生物

Pseudomonas fluorescens
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (185.64 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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

查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

=

浓度

×

体积

×

分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×

体积 (start)

V1

=

浓度 (final)

C2

×

体积 (final)

V2

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

  • 方案 二

    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); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL（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。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

  • 方案 三

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 1.25 mg/mL (2.32 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    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。

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动物溶解方案

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：
%

DMSO +

% 

%

Tween-80 +

%

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO， ，均可在 Shanghai Jinpan Biotech Co Ltd 网站选购。 ，Tween 80，均可在 Shanghai Jinpan Biotech Co Ltd 网站选购。

计算结果
工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 98.05%

Data Sheet (622 KB) SDS (252 KB)

COA (261 KB) HNMR (263 KB) RP-HPLC (226 KB) MS (198 KB)

产品使用指南 (1538 KB)

参考文献

  • [1]. 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]

    [2]. 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]

    [3]. 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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