Ketohexokinase inhibitor 1
目录号 : GC31400
Ketohexokinaseinhibitor1是一种己酮糖激酶(ketohexokinase(KHK))抑制剂，对KHK-C和KHK-A的IC50值分别为8.4nM和66nM，摘自专利US20170183328A1，example4。
Cas No.:2102501-84-6
Sample solution is provided at 25 µL, 10mM.
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Ketohexokinase inhibitor 1 is an inhibitor of ketohexokinase (KHK), with IC50s of 8.4 nM and 66 nM for KHK-C and KHK-A, respectively, extracted from patent US 20170183328 A1, example 4.
Ketohexokinase inhibitor 1 (Example 4) is an inhibitor of ketohexokinase (KHK), with IC50s of 8.4 nM and 66 nM for KHK-C and KHK-A, sepctively[1].
[1]. SUBSTITUTED 3-AZABICYCLO[3.1.0]HEXANES AS KETOHEXOKINASE INHIBITORS. US 20170183328 A1
Kinase experiment: | A 384-well format on a assay plate is used in the assay and monitored by UV-vis spectroscopy in continuous mode at room temperature (rt). Compounds (Ketohexokinase inhibitor 1) are prepared in DMSO as 4 mM stocks, diluted using an 11-point half-log scheme on a Biomek FX, and incubated at rt for 30 minutes with the reaction mixture containing 50 mM HEPES, pH 7.4, 140 mM KCl, 3.5 mM MgCl2, 0.8 mM fructose, 2 mM TCEP, 0.8 mM PEP, 0.7 mM NADH, 0.01% Triton X-100, 30 U/mL pyruvate kinase-lactate dehydrogenase, and 10 nM purified KHK-C. The compound concentration in each well ranged from 1 nM to 100 μM. The reaction is initiated with the addition of 0.2 mM ATP. The absorbance is measured for 30 minutes on a SpectraMax reader after ATP is added. The concentrations provided are based on the final mixture volume of 40 μL[1]. |
References: [1]. SUBSTITUTED 3-AZABICYCLO[3.1.0]HEXANES AS KETOHEXOKINASE INHIBITORS. US 20170183328 A1 | |
| Cas No. | 2102501-84-6 | SDF | |
| Canonical SMILES | O=C(C[C@H]1[C@@]2(CN(C[C@]12[H])C3=NC(N4[C@H](CC4)C)=NC(C(F)(F)F)=C3)[H])O | ||
| 分子式 | C16H19F3N4O2 | 分子量 | 356.34 |
| 溶解度 | DMS : ≥ 125 mg/mL (350.79 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 | 2.8063 mL | 14.0315 mL | 28.0631 mL |
| 5 mM | 0.5613 mL | 2.8063 mL | 5.6126 mL |
| 10 mM | 0.2806 mL | 1.4032 mL | 2.8063 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