LY451395
(Synonyms: LY451395) 目录号 : GC13010LY451395 (LY451395) 是一种有效且高度选择性的 AMPA 受体增强剂。
Cas No.:375345-95-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
LY451395 (Mibampator) is a powerful, highly selective and biarylsulfonamide potentiator of AMPA receptors [1].
LY451395 (Mibampator) has been found to be a potent, selective and centrally active positive allosteric modulators of AMPA receptor-mediated neurotransmission, which enhances ion channel flux in the presence of agonist by inhibiting desensitization and deactivation of the receptors. In addition, LY451395 has been revealed to enhance synaptic transmission. Besides, LY451395 has been reported to attenuate the response to acute ethanol administration in the rat in vivo [1]. Moreover, the in vivo metabolisms of LY451395 in mouse, rat, dog and human have produced several phase 1 oxidative metabolites [2].
References:
[1] Jones N1, Messenger MJ, O'Neill MJ, Oldershaw A, Gilmour G, Simmons RM, Iyengar S, Libri V, Tricklebank M, Williams SC. AMPA receptor potentiation can prevent ethanol-induced intoxication. Neuropsychopharmacology. 2008 Jun;33(7):1713-23. Epub 2007 Sep 12.
[2] Zmijewski M1, Gillespie TA, Jackson DA, Schmidt DF, Yi P, Kulanthaivel P. Application of biocatalysis to drug metabolism: preparation of mammalian metabolites of a biaryl-bis-sulfonamide AMPA (alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid) receptor potentiator using Actinoplanes missouriensis. Drug Metab Dispos. 2006 Jun;34(6):925-31. Epub 2006 Feb 28.
Cas No. | 375345-95-2 | SDF | |
别名 | LY451395 | ||
分子式 | C21H30N2O4S2 | 分子量 | 438.6 |
溶解度 | DMSO : ≥ 25 mg/mL (57.00 mM) | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.28 mL | 11.3999 mL | 22.7998 mL |
5 mM | 0.456 mL | 2.28 mL | 4.56 mL |
10 mM | 0.228 mL | 1.14 mL | 2.28 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。