Milbemycin A4 oxime
(Synonyms: 美倍霉素肟A4) 目录号 : GC44195
Milbemycin A4 oxime是一种通过氧化和肟化米尔贝霉素A4制备的半合成大环内酯类化合物，被用于治疗寄生虫相关疾病。
Cas No.:93074-04-5
Sample solution is provided at 25 µL, 10mM.
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Milbemycin A4 oxime is a semi-synthetic macrolide compound prepared by the oxidation and oximation of milbemycin A4, used for the treatment of parasitic diseases[1-2]. Milbemycin A4 oxime acts by activating glutamate-sensitive chloride channels in invertebrate neurons, leading to cell hyperpolarization and blockade of signal transmission, thereby causing paralysis and death of parasites[3-4].
In vitro, treatment of adriamycin-resistant human breast cancer cells MCF-7/adr with Milbemycin A4 oxime (0.1-5μM) in combination with adriamycin for 48 hours, Milbemycin A4 oxime significantly enhanced the cytotoxicity of adriamycin and reduced multidrug resistance in the cells[5].
In vivo, intraperitoneal administration of Milbemycin A4 oxime (0.5-2.5mg/kg/day) for 7 days in BALB/c mice with systemic Candida glabrata or Candida albicans infections, Milbemycin A4 oxime significantly reduced fungal loads in the spleen and kidneys[6].
References:
[1] Walker B, Izumikawa K, Tsai HF, et al. Milbemycin A4 oxime as a probe of azole transport in Candida glabrata. FEMS Yeast Res. 2014 Aug;14(5):755-61. doi: 10.1111/1567-1364.12164.
[2] Schares G, Hofmann B, Zahner H. Antifilarial activity of macrocyclic lactones: comparative studies with ivermectin, doramectin, milbemycin A4 oxime, and moxidectin in Litomosoides carinii, Acanthocheilonema viteae, Brugia malayi, and B. pahangi infection of Mastomys coucha. Trop Med Parasitol. 1994 Jun;45(2):97-106.
[3] Prichard RK. Macrocyclic lactone resistance in Dirofilaria immitis: risks for prevention of heartworm disease. Int J Parasitol. 2021 Dec;51(13-14):1121-1132.
[4] Mueller RS. An update on the therapy of canine demodicosis. Compend Contin Educ Vet. 2012 Apr;34(4):E1-4.
[5] Xiang W, Gao A, Liang H, et al. Reversal of P-glycoprotein-mediated multidrug resistance in vitro by milbemycin compounds in adriamycin-resistant human breast carcinoma (MCF-7/adr) cells. Toxicol In Vitro. 2010 Sep;24(6):1474-81.
[6] Silva LV, Sanguinetti M, Vandeputte P, et al. Milbemycins: more than efflux inhibitors for fungal pathogens. Antimicrob Agents Chemother. 2013 Feb;57(2):873-86.
Milbemycin A4 oxime是一种通过氧化和肟化米尔贝霉素A4制备的半合成大环内酯类化合物，被用于治疗寄生虫相关疾病[1-2]。Milbemycin A4 oxime通过激活无脊椎动物神经元中的谷氨酸敏感性氯离子通道，导致细胞超极化并阻滞信号传递，从而使寄生虫麻痹死亡[3-4]。
在体外，Milbemycin A4 oxime（0.1-5μM）与阿霉素联合处理阿霉素耐药的人乳腺癌细胞MCF-7/adr 48小时，显著增强阿霉素的细胞毒性，并降低细胞的多要耐药性[5]。
在体内，Milbemycin A4 oxime（0.5-2.5mg/kg/day）腹腔注射治疗7天，用于处理BALB/c小鼠系统性光滑念珠菌或白色念珠菌感染。Milbemycin A4 oxime显著降低了脾脏和肾脏中的真菌负荷[6]。
| Cell experiment [1]: | |
Cell lines | MCF-7 cells (drug-sensitive human breast carcinoma cell line) and MCF-7/adr cells (adriamycin-resistant human breast carcinoma cell line) |
Preparation Method | MCF-7 and MCF-7/adr cells were cultured in RPMI-1640 medium supplemented with 10% fetal calf serum at 37°C, 5% CO₂. MCF-7/adr cells were treated with Milbemycin A4 oxime at concentrations of 0.1, 1, and 5µM for 24-48 hours. |
Reaction Conditions | 0.1-5μM; 24-48h |
Applications | Milbemycin A4 oxime (5µM) significantly increased the cytotoxicity of adriamycin in MCF-7/adr cells. |
| Animal experiment [2]: | |
Animal models | BALB/c mice |
Preparation Method | Mice were intraperitoneally administered Milbemycin A4 oxime at dosages of 0.5 or 2.5mg/kg/day for 7 days. Mice were infected via lateral tail vein injection with C. glabrata (4×10⁷CFU) or C. albicans (7×10⁷CFU) strains. Mice were sacrificed 7 days post-infection for tissue burden analysis. |
Dosage form | 0.5-2.5mg/kg; i.p.; Daily injections for 7 days. |
Applications | Milbemycin A4 oxime significantly decreased fungal burdens in the spleen and kidneys of mice infected with either Candida glabrata or Candida albicans. |
References: | |
| Cas No. | 93074-04-5 | SDF | |
| 别名 | 美倍霉素肟A4 | ||
| Canonical SMILES | CC[C@H]([C@@H](C)CC1)O[C@]21C[C@](OC([C@@]3([H])[C@@]4(O)[C@@]5([H])/C(C(C)=C3)=N/O)=O)([H])C[C@](C/C=C(C)/C[C@@H](C)/C=C/C=C4\CO5)([H])O2 | ||
| 分子式 | C32H45NO7 | 分子量 | 555.7 |
| 溶解度 | DMF: soluble,DMSO: soluble,Ethanol: soluble,Methanol: soluble | 储存条件 | Store at -20°C, protect from light |
| 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 | 1.7995 mL | 8.9977 mL | 17.9953 mL |
| 5 mM | 359.9 μL | 1.7995 mL | 3.5991 mL |
| 10 mM | 180 μL | 899.8 μL | 1.7995 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet