GKA50 |
Catalog No.GC38784
One-Click Copy Product Info
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GKA50은 강력한 글루코키나제 활성제(EC50=33 nM at 5 mM 포도당)이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 851884-87-2
Sample solution is provided at 25 µL, 10mM.
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GKA50은 강력한 글루코키나제 활성제(EC₅₀=5 mM 포도당에서 33 nM)이다. GKA50은 쥐 랑게르한스섬과 MIN6 세포에서 인슐린 분비를 촉진한다. GKA50은 고지방 식이를 한 암컷 쥐에서 유의한 혈당 강하 효과를 보여준다 [1][2].
GKA50(0.01-100 μM; 24시간)은 EC₅₀ 값이 1~2 μM인 INS-1 세포 증식을 촉진한다 [2].GKA50(1.2 μM+40 μM 포도당; 2-4일) 처리는 만성 고혈당에 의해 유도된 INS-1 세포의 사멸을 줄인다 [2].GKA50은 인간 글루코키나제 효소 활성을 활성화해서 EC₅₀은 0.022 μM이다.GKA50은 췌장 인슐리노마 세포 라인 INS-1에서 인슐린 분비를 촉진하고 EC₅₀은 0.065 μM이다.GKA50은 글루코키나제와 사멸 단백질 BAD를 조절해서 만성 고혈당에 의해 유도된 사멸을 줄인다 [2].세포 증식 검사 [2]세포 라인: INS-1 세포(3 μM 포도당으로 밤새 굶기)
GKA50(1-30 mg/kg; 경구)은 경구 포도당 내성 검사에서 유의한 혈당 강하 효과를 나타낸다 [1].동물 모델: 고지방 식이를 한 비만 암컷 주커(fa/fa) 쥐 [1]
References:
[1]. Coope GJ, et al. Predictive blood glucose lowering efficacy by Glucokinase activators in high fat fed female Zucker rats. Br J Pharmacol. 2006 Oct;149(3):328-35.
[2]. McGlasson L, et al. The glucokinase activator GKA50 causes an increase in cell volume and activation of volume-regulated anion channels in rat pancreatic β-cells. Mol Cell Endocrinol. 2011 Aug 6;342(1-2):48-53.
| Cas No. | 851884-87-2 | SDF | |
| Canonical SMILES | O=C(C1=CC=C(NC(C2=CC(O[C@@H](C)CC3=CC=CC=C3)=CC(O[C@@H](C)COC)=C2)=O)N=C1)O | ||
| Formula | C26H28N2O6 | M.Wt | 464.51 |
| Solubility | DMSO : 46 mg/mL (99.03 mM; Need ultrasonic and warming) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1528 mL | 10.764 mL | 21.5281 mL |
| 5 mM | 430.6 μL | 2.1528 mL | 4.3056 mL |
| 10 mM | 215.3 μL | 1.0764 mL | 2.1528 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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 saline, 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)