Ivermectin B1a
(Synonyms: 伊维菌素 B1a) 目录号 : GC12700
An anthelmintic
Cas No.:71827-03-7
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
Ivermectin B1a is the main component (not less than 80%) of the anthelmintic, ivermectin. Ivermectin is one of the most useful veterinary antiparasitic drugs ever produced. Ivermectin belongs to the macrocyclic lactone class of avermectins. Ivermectin contains two homologous compounds, H2B1a and H2B1b. Avermectins are potent insecticidal, anthelmintic and acaricidal compounds in mediating the paralysis of nematodes and certain classes of ectoparasites by increasing the membrane permeability to chlorine ions[1].
In humans, ivermectin has been used to treat African river blindness (onchocerciasis). Ivermectin significantly decreased the prevalence of skin and eye diseases linked to this infection [2]. Ivermectin B1a produced antiparasitic activity via an interaction with a common receptor molecule, glutamate-gated chloride channels, which virtually expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function. The EC50 of ivermectin was 104 nM [1,3].
References:
[1] J. Wolsetnholme and A. T. Rogers. Glutamate-gated chloride channels and the mode of action of the avermectin/milbemycin anthelmintics. Parasitology131 Suppl, S85-S95 (2005).
[2] S. Gaisser, L. Kellenberger, A. L. Kaja, et al. Direct production of ivermectin-like drugs after domain exchange in the avermectin polyketide synthase of Streptomyces avermitilis ATCC31272. Organic & Biomolecular Chemistry 1(16), 2840-2847 (2003).
[3] J. P. Arena, K. K. Liu, P. S. Paress, et al. The mechanism of action of avermectins in Caenorhabditis elegans: Correlation between activation of glutamate-sensitive chloride current, membrane binding, and biological activity. Journal of Parasitology 81, 286-294 (1995).
| Cas No. | 71827-03-7 | SDF | |
| 别名 | 伊维菌素 B1a | ||
| 化学名 | 5-O-demethyl-22,23-dihydro-avermectin A1a | ||
| Canonical SMILES | C/C([C@@H](O[C@@]1([H])C[C@H](OC)[C@@H](O[C@]2([H])O[C@@H](C)[C@H](O)[C@@H](OC)C2)[C@H](C)O1)[C@@H](C)/C=C/C=C(CO3)/[C@@]([C@@]3([H])[C@H](O)C(C)=C4)(O)[C@]4([H])C5=O)=C\C[C@]6([H])C[C@@](O5)([H])C[C@]7(CC[C@H](C)[C@]([C@H](CC)C)([H])O7)O6 | ||
| 分子式 | C48H74O14 | 分子量 | 875.1 |
| 溶解度 | DMSO : 100 mg/mL (114.27 mM; Need ultrasonic) | 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 | 1.1427 mL | 5.7136 mL | 11.4273 mL |
| 5 mM | 0.2285 mL | 1.1427 mL | 2.2855 mL |
| 10 mM | 0.1143 mL | 0.5714 mL | 1.1427 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。