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FGH10019

Catalog No.GC31323

FGH10019는 IC50이 1μM인 새로운 스테롤 조절 요소 결합 단백질(SREBP) 억제제입니다.

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FGH10019 Chemical Structure

Cas No.: 1046045-61-7

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$117.00
재고 있음
1mg
US$57.00
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5mg
US$143.00
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10mg
US$197.00
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25mg
US$311.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Description of FGH10019

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.

Protocol of FGH10019

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.

Chemical Properties of FGH10019

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
Solubility 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.

Complete Stock Solution Preparation Table of FGH10019

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.6774 mL 13.3872 mL 26.7745 mL
5 mM 0.5355 mL 2.6774 mL 5.3549 mL
10 mM 0.2677 mL 1.3387 mL 2.6774 mL
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In vivo Formulation Calculator (Clear solution) of FGH10019

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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.

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리뷰

Review for FGH10019

Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

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