3-TYP |
| Katalog-Nr.GC19013 |
3-TYP hemmt SIRT3 mit einem IC50-Wert von 16 nM und ist gegenüber SIRT1 und SIRT2 mit IC50-Werten von 88 nM bzw. 92 nM potenter.
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Cas No.: 120241-79-4
Sample solution is provided at 25 µL, 10mM.
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3-TYP hemmt SIRT3 mit einem IC50-Wert von 16 nM und ist gegenüber SIRT1 und SIRT2 mit IC50-Werten von 88 nM bzw. 92 nM potenter.[1]
In vitro hat 50 μM 3-TYP die barriere-schützende Wirkung von PD in mehreren Organen septischer Mäuse aufgehoben. In HUVECs verringerte 3-TYP (50 μM) den durch PD vermittelten Schutz gegen die Umverteilung von F-Aktin, die Dissoziation des Cadherin-Catenin-Komplexes und die Hyperpermeabilität der Endothelmonoschicht.[3] Eine in vitro-Studie zeigte, dass 3-TYP bei 100 µM die Expression von Genen, die an der Lipolyse und dem Glukosetransport GLUT4 beteiligt sind, im Vergleich zu HNK verringerte. Gleichzeitig verursachte 3-TYP auch einen Anstieg der Genexpression von adipocyten-spezifischen Zytokinen, einschließlich IL6, Resistin und TNF-α. In vitro hemmte die Behandlung mit 100 µM 3-TYP offensichtlich die Glukoseaufnahme in 3T3-L1-Adipozyten im Vergleich zur Kontrolle in Anwesenheit von Insulin.[5] In A/R-behandelten H9c2-Zellen führte die Behandlung mit 4-P-PDOT (10 μM) und 3-TYP (5 μM) zu keinem bemerkenswerten Unterschied in der Zellviabilität. Darüber hinaus erhöhte die Kombination von 4-P-PDOT und 3-TYP die apoptotische Signalgebung durch Erhöhung der gespaltenen Caspase-3- und Bax-Expression, während die Bcl-2-Expression im Vergleich zur A/R + Mel-Gruppe verringert wurde.[6]
Ein in vivo-Experiment zeigte, dass die Behandlung mit 50 mg/kg intraperitoneal 3-TYP die Induktion der Mitophagie durch Verringerung der Expressionsniveaus von FOXO3α, BINP3, LC3-II/LC3-I, SOD2, PRDX3 und P62 umkehrte.[2] Ein in vivo-Wirksamkeitstest zeigte, dass bei C57BL/6-Mäusen die Verabreichung von 50 mg/kg 3-TYP die antioxidativen Effekte von TBM aufhob.[4]
References:
[1].Pi H, et al. SIRT3-SOD2-mROS-dependent autophagy in cadmium-induced hepatotoxicity and salvage by melatonin. Autophagy. 2015;11(7):1037-51.
[2].Yu W, et al. Dexmedetomidine Ameliorates Hippocampus Injury and Cognitive Dysfunction Induced by Hepatic Ischemia/Reperfusion by Activating SIRT3-Mediated Mitophagy and Inhibiting Activation of the NLRP3 Inflammasome in Young Rats. Oxid Med Cell Longev. 2020 Nov 20;2020:7385458.
[3].Wu J, et al. Polydatin protects against lipopolysaccharide-induced endothelial barrier disruption via SIRT3 activation. Lab Invest. 2020 Apr;100(4):643-656.
[4].Lv D, et al. Tubeimoside I Ameliorates Myocardial Ischemia-Reperfusion Injury through SIRT3-Dependent Regulation of Oxidative Stress and Apoptosis. Oxid Med Cell Longev. 2021 Nov 9;2021:5577019.
[5]. Lee AY, et al. Sirt3 Pharmacologically Promotes Insulin Sensitivity through PI3/AKT/mTOR and Their Downstream Pathway in Adipocytes. Int J Mol Sci. 2022 Mar 29;23(7):3740.
[6].Wu J, et al. Melatonin Attenuates Anoxia/Reoxygenation Injury by Inhibiting Excessive Mitophagy Through the MT2/SIRT3/FoxO3a Signaling Pathway in H9c2 Cells. Drug Des Devel Ther. 2020 May 25;14:2047-2060.
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were pretreated with 3-TYP (50 μM) or the vehicle for 1 h, followed by the treatment with DHM (20 μM) for 2 h and 0.2 mM of PA for 16 h. |
Reaction Conditions | 50 μM, 16h |
Applications | DHM treatment attenuates PA-induced autophagy arrest and oxidative stress in hepatocytes, which was mediated via SIRT3. |
| Animal experiment [2]: | |
Animal models | C57BL/6 J male mice |
Preparation Method | Both 3-TYP and 2-methoxyestradiol were administered by intraperitoneal injection starting 1 week prior to NE for 7 days 3-TYP was administered at 50 mg/kg/day, and 2-ME was administered at 16 mg/kg/day. |
Dosage form | 50 mg/kg/day,i.p. |
Applications | 3-TYP exacerbates noise-induced hair cell damage; 3-TYP increases the acetylation level of SOD2 and aggravates oxidative stress and apoptosis. |
References: | |
| Cas No. | 120241-79-4 | SDF | |
| Canonical SMILES | C1(C2=CN=NN2)=CC=CN=C1 | ||
| Formula | C7H6N4 | M.Wt | 146.15 |
| Löslichkeit | DMSO : 100 mg/mL (684.23 mM);Ethanol : 16.67 mg/mL (114.06 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 | 6.8423 mL | 34.2114 mL | 68.4229 mL |
| 5 mM | 1.3685 mL | 6.8423 mL | 13.6846 mL |
| 10 mM | 0.6842 mL | 3.4211 mL | 6.8423 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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