FGH10019 |
| رقم الكتالوجGC31323 |
FGH10019 هو مثبط جديد لبروتين رابط لعنصر الستيرول (SREBP) مع IC 50 من 1 ميكرومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1046045-61-7
Sample solution is provided at 25 µL, 10mM.
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FGH10019 is a novel sterol regulatory element-binding protein (SREBP) inhibitor with IC50 of 1 μM.
Treatment of the CHO-K1 cells with analog FGH10019 decreases the percentage of the mature form of SREBP-2 (68 kDa) at lower concentrations than treatment with fatostatin. Densitometric analysis of the gels indicates that the IC50 of analog FGH10019 is approximately 1 μM, which is 5-10 times lower than the IC50 of fatostatin (appr 10 μM)[1].
FGH10019-treated chow is fed at a dose rate calculated to provide about 0.7 mg analog FGH10019 per day, at about 23 mg/kg body weight, to 5-wk-old male ob/ob mice weighing an average of appr 30 g. After 8 wk on the analog 24-treated chow, the mice gain 8-9 % less weight than control mice[1].
[1]. Kamisuki S, et al. Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins. J Med Chem. 2011 Jul 14;54(13):4923-7.
Animal experiment: | Five-week-old homozygous male obese (ob/ob) mice (C57BL/6J) are housed five per cage, and had ad libitum access to normal chow and water for 1 wk after their arrival. On day 1 of the experiment, the animals (10 per group) are fed normal chow (control diet) or chow that contains 200 mg/kg of analogue 24. These doses are estimated to provide approximately 0.7 mg analogue 24 per day (appr 23 mg/kg body weight per day). Daily food intake and body weight are carefully monitored and recorded between 3:00 and 5:00 p.m. Serum constituents, and TG levels in livers are determined. |
References: [1]. Kamisuki S, et al. Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins. J Med Chem. 2011 Jul 14;54(13):4923-7. | |
| Cas No. | 1046045-61-7 | SDF | |
| Canonical SMILES | CS(=O)(NC1=CC=C(C2=CSC(C3=CC(CCC)=NC=C3)=N2)C=C1)=O | ||
| Formula | C18H19N3O2S2 | M.Wt | 373.49 |
| الذوبان | DMSO : ≥ 38 mg/mL (101.74 mM) | 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 | 2.6774 mL | 13.3872 mL | 26.7745 mL |
| 5 mM | 535.5 μL | 2.6774 mL | 5.3549 mL |
| 10 mM | 267.7 μL | 1.3387 mL | 2.6774 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
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- 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.)
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