3-TYP |
| Catalog No.GC19013 |
3-TYP inhibit SIRT3 with an IC50 of 16 nM, and is more potent over SIRT1 and SIRT2 with IC50 of 88 nM and 92 nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 120241-79-4
Sample solution is provided at 25 µL, 10mM.
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3-TYP inhibit SIRT3 with an IC50 of 16 nM, and is more potent over SIRT1 and SIRT2 with IC50 of 88 nM and 92 nM, respectively.[1]
In vitro, with 50 μM 3-TYP abrogated the barrier protective effect of PD in multiple organs of septic mice. In HUVECs, 3-TYP (50 μM) diminished PD-mediated protection against F-actin redistribution, cadherin–catenin complex dissociation, and endothelial monolayer hyperpermeability.[3] In vitro study it demonstrated that at 100 µM, 3-TYP decreased expression of genes involved in lipolysis and glucose transport GLUT4 compared to HNK. At the meantime, 3-TYP also caused an increase in gene expression of adipocyte-specific cytokines, including IL6, resistin, and TNF-α. In vitro, treatment with 100 µM 3-TYP obviously inhibited glucose uptake in 3T3-L1 adipocytes in contrast to control in the presence of insulin.[5] In A/R-treated H9c2 cells, 4-P-PDOT (10 μM) and 3-TYP (5 μM) treatment resulted in no notable difference in cell viability. In addition, combination wiith 4-P-PDOT and 3-TYP elevated apoptotic signaling by increasing cleaved caspase-3 and Bax expression while decreasing Bcl-2 expression compared with that in the A/R + Mel group.[6]
In vivo experiment it suggested that treatment with 50 mgkg intraperitoneally 3-TYP reversed the induction of mitophagy by decreasing the expression levels of FOXO3α, BINP3, LC3-II/LC3-I, SOD2, PRDX3, and P62.[2] In vivo efficacy test it indicated that C57BL/6 mice were administrated 50 mg/kg 3-TYP abolished TBM's antioxidative effects.[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 |
| Solubility | 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. |
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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 | |||
|
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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μL
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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.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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