Evans Blue tetrasodium salt
(Synonyms: 伊文思蓝; Direct Blue 53; C.I. 23860) 目录号 : GC13947
Evans Blue tetrasodium salt 是通过膜结合兴奋性氨基酸转运蛋白 (EAAT) 摄取 L-谷氨酸的有效抑制剂。
Cas No.:314-13-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 220 and 150 nM for GluRl and GIuR6, respectively.
Evans Blue tetrasodium salt is a potent inhibitor of AMPA and kainate receptor-mediated currents (GluRl and GIuR6).
Pharmacologically, the glutamate transporter is specific for glutamate and the closely related analogue L-aspartate does not block the uptake, whereas agents like L-homocysteate and La- aminoadipate block the vesicular L-glutamate uptake poorly.
In vitro: Evans blue inhibits the kainate-mediated responses of the non-NMDA receptor subunits (GIuRl, G1uR1,2, G1uRl,3, and G1uR2,3) expressed in Xenopus oocytes without the response of GluR3 and G1uR6 at low concentrations (IC50= 355 nM for the subunit combination GluR1,2). This pocess was partially reversible without competing with kainate for the agonist binding site [1]. In whole-cell patch clamp recordings of transfected human embryonic kidney 293 cells, Evans blue is a potent inhibitor of glutamate-evoked currents mediated by the kainate-type receptor GIuR6 as long as the AMPA-type receptor GluRl. Interestingly, pretreating with the lectin concanavalin cells recorded relatively little EB inhibition of GIuR6 currents, eliminating kainate receptor desensitization. In addition to decreasing GluR6-mediated peak current amplitude, EB significantly changed receptor desensitization by slowing the rate of onset by ~2-fold (1 M EB) and the rate of recovery by ~2-fold (0.1 p.M EB), and enhancing the steady state to peak current amplitude ratio by ~50-fold (1 M EB) [2].
In vivo: So far, no study in vivo has been conducted.
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Roseth S, Fykse EM, Fonnum F. Uptake of L-glutamate into rat brain synaptic vesicles: effect of inhibitors that bind specifically to the glutamate transporter. J Neurochem. 1995 Jul;65(1):96-103.
[2] Price CJ, Raymond LA. Evans blue antagonizes both alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate and kainate receptors and modulates receptor desensitization. Mol Pharmacol. 1996 Dec; 50 (6):1665-71.
| Cas No. | 314-13-6 | SDF | |
| 别名 | 伊文思蓝; Direct Blue 53; C.I. 23860 | ||
| 化学名 | sodium (6Z,6'Z)-6,6'-(2,2'-(3,3'-dimethyl-[1,1'-biphenyl]-4,4'-diyl)bis(hydrazin-2-yl-1-ylidene))bis(4-amino-5-oxo-5,6-dihydronaphthalene-1,3-disulfonate) | ||
| Canonical SMILES | O=C1C(C(C=C/C1=N/NC(C(C)=C2)=CC=C2C3=CC=C(C(C)=C3)N/N=C4C(C(C(C=C\4)=C5S([O-])(=O)=O)=C(C(S([O-])(=O)=O)=C5)N)=O)=C6S([O-])(=O)=O)=C(C(S([O-])(=O)=O)=C6)N.[Na+].[Na+].[Na+].[Na+] | ||
| 分子式 | C34H24N6Na4O14S4 | 分子量 | 960.82 |
| 溶解度 | ≥ 192.4 mg/mL in DMSO, ≥ 213.8 mg/mL in Water | 储存条件 | Store at RT |
| 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 | 1.0408 mL | 5.2039 mL | 10.4078 mL |
| 5 mM | 0.2082 mL | 1.0408 mL | 2.0816 mL |
| 10 mM | 0.1041 mL | 0.5204 mL | 1.0408 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。