Dimebolin
(Synonyms: 2,3,4,5-四氢-2,8-二甲基-5-[2-(6-甲基吡啶-3-基)乙基]-1H-吡啶并[4,3-B]吲哚,Dimebon?) 目录号 : GC15723
A neuroprotective agent
Cas No.:3613-73-8
Sample solution is provided at 25 µL, 10mM.
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Dimebolin is an orally-available antihistamine drug with a long history of clinical use in Russia [1][2][3][4].
Dimebolin has been proposed to be useful for treating neurodegenerative disorders, including Alzheimer's disease (AD) and Huntington's disease (HD). Dimebon might exhibit efficacy by blocking NMDA receptors or voltage-gated Ca2+ channels and by preventing mitochondrial permeability pore transition [3].
Dimebolin is an orally-available antihistamine drug. Dimebon improved survival of cerebellar granule cells during long-term incubation with Aβ25-35. Dimebolin also blocked potential-dependent Ca(2+) entry into neurons by about 20% by blocking L-type Ca(2+) channels [4]. In the cerebellum cell culture, Dimebolin protected neurons against the neurotoxic action of Aβ25-35 with EC50 value of 25 μM. On isolated rat ileum intestine, Dimebolin displayed Ca2+-blocking properties with IC50 value of 57 μM. Dimebon also exhibited anticholinesterase activity with IC50 values of 7.9 μM and 42 μM for butyryl-choline esterase and acetylcholine esterase, respectively [5].
In rats treated with the neurotoxin AF64A, Dimebolin exhibited cognition and memory-enhancing properties. In mice, Dimebolin prevented NMDA-induced seizures with EC50 value of 42 ± 6 mg/kg [5].
References:
[1]. Lermontova NN, Lukoyanov NV, Serkova TP, et al. Dimebon improves learning in animals with experimental Alzheimer's disease. Bull Exp Biol Med. 2000 Jun;129(6):544-6.
[2]. Doody RS, Gavrilova SI, Sano M, et al. Effect of dimebon on cognition, activities of daily living, behaviour, and global function in patients with mild-to-moderate Alzheimer's disease: a randomised, double-blind, placebo-controlled study. Lancet. 2008 Jul 19;372(9634):207-15.
[3]. Wu J, Li Q, Bezprozvanny I. Evaluation of Dimebon in cellular model of Huntington's disease. Mol Neurodegener. 2008 Oct 21;3:15.
[4]. Lermontova NN, Redkozubov AE, Shevtsova EF, et al. Dimebon and tacrine inhibit neurotoxic action of beta-amyloid in culture and block L-type Ca(2+) channels. Bull Exp Biol Med. 2001 Nov;132(5):1079-83.
[5]. Bachurin S, Bukatina E, Lermontova N, et al. Antihistamine agent Dimebon as a novel neuroprotector and a cognition enhancer. Ann N Y Acad Sci. 2001 Jun;939:425-35.
| Cas No. | 3613-73-8 | SDF | |
| 别名 | 2,3,4,5-四氢-2,8-二甲基-5-[2-(6-甲基吡啶-3-基)乙基]-1H-吡啶并[4,3-B]吲哚,Dimebon? | ||
| 化学名 | 2,3,4,5-tetrahydro-2,8-dimethyl-5-[2-(6-methyl-3-pyridinyl)ethyl]-1H-pyrido[4,3-b]indole | ||
| Canonical SMILES | CC1=CC=C(N(CCC2=CC=C(C)N=C2)C3=C4CN(C)CC3)C4=C1 | ||
| 分子式 | C21H25N3 | 分子量 | 319.4 |
| 溶解度 | ≤30mg/ml in ethanol;1mg/ml in DMSO;3mg/ml in dimethyl formamide | 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 | 3.1309 mL | 15.6544 mL | 31.3087 mL |
| 5 mM | 0.6262 mL | 3.1309 mL | 6.2617 mL |
| 10 mM | 0.3131 mL | 1.5654 mL | 3.1309 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