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Purity: ≥98%
3-TYP [3TYP; full/chemical name: 3-(1H-1,2,3-triazol-4-yl) pyridine)] is a novel, potent and selective SIRT3 inhibitor (IC50 = 16 nM) with high selectivity for SIRT3 over SIRT1 (IC50=88 nM) and SIRT2 (IC50=92 nM). 3-TYP inhibited SIRT3-SOD2 signaling, which prevented the melatonin-mediated suppression of autophagy. Notably, melatonin increased SIRT3 activity in vivo to inhibit Cd-induced autophagic cell death. These findings indicate that melatonin, which is dependent on the SIRT3/SOD2 pathway, has a hepatoprotective effect on mitochondrial-derived O2(•-)-stimulated autophagic cell death.
| Targets |
SIRT3 ( IC50 = 16 nM ); SIRT1 ( IC50 = 88 nM ); SIRT2 ( IC50 = 92 nM )
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| Cell Assay |
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| Animal Protocol |
In brief, a 6-0 silk suture slipknot is wrapped around the left anterior descending coronary artery to temporarily exteriorize the heart in male C57BL/6 mice under 2% isoflurane anesthesia. Following 30 minutes of myocardial ischemia, the myocardium is reperfused for 3 hours (to measure oxidative stress and perform a western blot analysis) or 24 hours (to assess infarct size, cardiac function, and apoptotic index). The slipknot is then released. The identical surgical procedures are performed on sham-operated mice, with the exception that the suture under the left coronary artery is left untied. Mice are randomized to receive an intraperitoneal injection of either melatonin (20 mg/kg) or vehicle (1% ethanol) ten minutes prior to reperfusion. The C57BL/6 mice are split into the following groups at random: (i) Sham group: mice underwent the sham operation and are treated with vehicle (1% ethanol); (ii) Mel group: mice are treated with melatonin (20 mg/kg via intraperitoneal injection); (iii) IR+V group: mice underwent the MI/R operation and are treated with vehicle (1% ethanol); (iv) IR+Mel group: mice underwent the MI/R operation and are treated with melatonin (20 mg/kg via intraperitoneal injection 10 minutes before reperfusion); (v) IR+Mel+3-TYP group: mice are pretreated with 3-TYP (3-TYP is intraperitoneally injected at a dose of 50 mg/kg every 2 days for a total of three doses prior to the MI/R surgery), subjected to the MI/R operation, and treated with melatonin (20 mg/kg via intraperitoneal injection 10 minutes before reperfusion); and (vi) IR+3-TYP group: mice are pretreated with 3-TYP and then subjected to the MI/R operation.
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| References |
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| Molecular Formula |
C7H6N4
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| Molecular Weight |
146.1493
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| Exact Mass |
146.06
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| Elemental Analysis |
C, 57.53; H, 4.14; N, 38.34
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| CAS # |
120241-79-4
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| Appearance |
Solid powder
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| SMILES |
C1=CC(=CN=C1)C2=NNN=C2
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| InChi Key |
VYXFEFOIYPNBFK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H6N4/c1-2-6(4-8-3-1)7-5-9-11-10-7/h1-5H,(H,9,10,11)
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| Chemical Name |
3-(2H-triazol-4-yl)pyridine
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| Synonyms |
3 TYP; 3-TYP; 3TYP
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 29~125 mg/mL (198.4~855.3 mM)
Water : ~1.3 mg/mL (~8.6 mM) Ethanol : 16.7~29 mg/mL (114.1~198.4 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (14.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (14.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (14.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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