UCPH-101
目录号 : GC19365
A noncompetitive inhibitor of EAAT1
Cas No.:1118460-77-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Cells are split into poly-D-lysine-coated black 96-well plates with clear bottom. At 16 to 24 h later, the medium is aspirated, and the cells are washed with 100 μL Krebs buffer [140 mM NaCl/4.7 mM KCl/2.5 mM CaCl2/1.2 mM MgCl2/11 mM HEPES/10 mM D-glucose, pH 7.4]; 50 μL Krebs buffer supplemented with various concentrations of UCPH-101 or TBOA is added to the wells, after which an additional 50 μL Krebs buffer supplemented with the FMP assay dye (1 mg/mL) is added to each well. The plate is incubated at 37°C in a humidified 5% CO2 incubator for 30 min and assayed in a reader measuring emission at 560 nm caused by excitation at 530 nm before and up to 1 min after addition of 33 μL Glu solution[1]. |
References: [1]. Abrahamsen B, et al. Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain. J Neurosci. 2013 Jan 16;33(3):1068-87. | |
UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 uM.
UCPH-101 and UCPH-102 inhibit EAAT1 anion currents in a concentration-dependent manner, with KD values of 0.34±0.03 uM (Hill=1.3±0.13, n≥9) for UCPH-101 and 0.17±0.02 uM (Hill=0.97±0.11, n≥7) for UCPH-102. A small but significant decrease in the total expression levels of both HA-EAAT1 and HA-GLAST is observed in cells preincubated with 100 uM UCPH-101 (p=0.048)[1].
References:
[1]. Abrahamsen B, et al. Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain. J Neurosci. 2013 Jan 16;33(3):1068-87.
| Cas No. | 1118460-77-7 | SDF | |
| Canonical SMILES | O=C(C1)C2=C(OC(N)=C(C#N)C2C3=CC=C(OC)C=C3)CC1C4=CC=CC5=C4C=CC=C5 | ||
| 分子式 | C27H22N2O3 | 分子量 | 422.48 |
| 溶解度 | DMSO : ≥ 110 mg/mL (260.37 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.367 mL | 11.8349 mL | 23.6698 mL |
| 5 mM | 0.4734 mL | 2.367 mL | 4.734 mL |
| 10 mM | 0.2367 mL | 1.1835 mL | 2.367 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。