Fructose 1,6-bisphosphatase-1 Inhibitor
(Synonyms: F1,6BPase-1 Inhibitor|FBP1 Inhibitor|FBPase-1 Inhibitor) 目录号 : GC16703
A gluconeogenesis inhibitor
Cas No.:883973-99-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 3.4 μM
Fructose 1,6-bisphosphatase-1 Inhibitor is a fructose 1,6-bisphosphatase-1 inhibitor.
Fructose 1,6-bisphosphatase-1 (FBPase-1), an enzyme catalyzing the conversion of fructose-1,6-bisphosphate to fructose 6-phosphate, is one of the rate-limiting steps in gluconeogenesis. Excess hepatic fructose 1,6-bisphosphatase-1 activity contributes to hyperglycemia in patients.
In vitro: In a confirmatory assay, production of fructose-6-phosphate was monitored to give 6-phosphoglucono-d-lactone. The concomitant reduction of NADP to NADPH was also monitored. Fructose 1,6-bisphosphatase-1 Inhibitor was found to exhibit similar potency in these two distinct assays of FBPase-1 activity. Moreover, the ‘coupled’ assay format produced time-resolved data that might be subjected to kinetic analysis, indicating a Ki of 1.1μM for Fructose 1,6-bisphosphatase-1 Inhibitor. Fructose 1,6-bisphosphatase-1 Inhibitor also functioned as expected in a cellular model of glucose production. In an assay, rat hepatoma cells were starved of nutrients, making them highly dependent on the processing of pyruvate and lactate. Glucose production was measured over a three-hour period and the decrease in glucose that occurs with increasing doses of Fructose 1,6-bisphosphatase-1 Inhibitor was indicative of its ability to block gluconeogenesis by inhibiting FBPase-1 [1].
In vivo: So far, there is no animal data reported.
Clinical trial: Up to now, Fructose 1,6-bisphosphatase-1 Inhibitor is still in the preclinical development stage.
Reference:
[1] C. Lai, R. J. Gum, M. Daly, et al. Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase. Bioorganic & Medicinal Chemistry Letters 16(7), 1807-1810 (2006).
| Cas No. | 883973-99-7 | SDF | |
| 别名 | F1,6BPase-1 Inhibitor|FBP1 Inhibitor|FBPase-1 Inhibitor | ||
| 化学名 | 2,5-dichloro-N-(5-chloro-2-benzoxazolyl)-benzenesulfonamide | ||
| Canonical SMILES | ClC1=CC=C2C(N=C(NS(C3=C(Cl)C=CC(Cl)=C3)(=O)=O)O2)=C1 | ||
| 分子式 | C13H7Cl3N2O3S | 分子量 | 377.6 |
| 溶解度 | ≤14mg/ml in DMSO;20mg/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 | 2.6483 mL | 13.2415 mL | 26.4831 mL |
| 5 mM | 0.5297 mL | 2.6483 mL | 5.2966 mL |
| 10 mM | 0.2648 mL | 1.3242 mL | 2.6483 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。
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