Fructose 1,6-bisphosphatase-1 Inhibitor (Synonyms: F1,6BPase-1 Inhibitor|FBP1 Inhibitor|FBPase-1 Inhibitor) |
| Catalog No.GC16703 |
프럭토스 1,6-비스포스파타제-1 억제제(화합물 1)는 프럭토스-1,6-비스포스파타제(FBPase-1)의 알로스테릭 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 883973-99-7
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
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 | |
| Synonyms | F1,6BPase-1 Inhibitor|FBP1 Inhibitor|FBPase-1 Inhibitor | ||
| Chemical Name | 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 | ||
| Formula | C13H7Cl3N2O3S | M.Wt | 377.6 |
| Solubility | ≤14mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *