| Size | Price | Stock | Qty |
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| 5mg |
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| 50mg |
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| Targets |
SRT1460 is a potent and selective activator of Sirtuin 1 (SIRT1), an NAD+-dependent deacetylase involved in the regulation of metabolism, aging, and stress responses. It has an EC1.5 of 2.9 μM for SIRT1 activation and shows >100-fold selectivity over SIRT2 and SIRT3 (EC1.5 > 300 μM). By activating SIRT1, SRT1460 modulates downstream signaling pathways involved in metabolism and cell survival. Its mechanism involves allosteric activation of SIRT1.
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| ln Vitro |
Cell viability was dilutedly decreased by SRT 1460 (2–6 μM; 72 hours), with all pancreas being more sensitive than control HPDE cells. These cells' IC50 values are as follows: 1.62±0.13 μM for Patu8988t; 2.31±0.23 μM for SU86.86; 0.66±0.02 μM for Panc-1; and 2.39±0.29 μM for HPDE[2]. The autophagy marker LC3-II rises in expression when exposed to SRT 1460 (5 μM) for 16 hours [2].
In vitro, SRT1460 is a potent and selective SIRT1 activator with an EC1.5 of 2.9 μM. It displays good selectivity for SIRT1 versus SIRT2 and SIRT3 (EC1.5 > 300 μM) and is more potent than Resveratrol. SRT1460 reduces cell viability and growth of pancreatic cancer cells and induces apoptosis. Its in vitro activity is characterized by potent SIRT1 activation and antiproliferative effects. |
| ln Vivo |
In vivo, SRT1460 improves insulin sensitivity, lowers plasma glucose, and increases mitochondrial capacity in obese mice models. It has been shown to have beneficial metabolic effects in animal models. However, detailed in vivo efficacy data for specific disease models are limited. SRT1460 is primarily used as a research tool for studying SIRT1 biology and metabolism.
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| Enzyme Assay |
In vitro enzyme assays for SRT1460 typically involve measuring the activation of SIRT1 deacetylase activity. The compound has an EC1.5 of 2.9 μM for SIRT1 activation. Its selectivity over SIRT2 and SIRT3 is also assessed using similar assays. These assays confirm its mechanism of action as a SIRT1 activator.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Patu8988t (pancreatic cancer cells), Panc-1 (pancreatic cancer cells), SU86.86 (pancreatic cancer cells), HPDE Cell Tested Concentrations: 2 μM, 4 μM, 6 μM Incubation Duration: Results at 72 hrs (hours): Inhibition of cell viability was dose-dependent, and all pancreatic cancer cells were more sensitive than control HPDE cells. The IC50 of these cells are: Patu8988t, 1.62±0.13 μM; SU86.86, 2.31±0.23 μM; Panc-1, 0.66±0.02 μM; HPDE, 2.39±0.29 μM. Western Blot Analysis[2] Cell Types: Patu8988t Cell Tested Concentrations: 5 μM Incubation Duration: 16 hrs (hours) Experimental Results: SRT1460 increases the expression of the autophagy marker LC3-II. In vitro cellular assays for SRT1460 typically involve treating cancer cell lines such as pancreatic cancer cells with the compound and measuring cell viability, proliferation, and apoptosis. SRT1460 reduces cell viability and growth of pancreatic cancer cells and induces apoptosis. These cell-based studies demonstrate its antiproliferative effects and its mechanism of action as a SIRT1 activator. |
| Animal Protocol |
In vivo animal models for SRT1460 include obese mice models to evaluate its metabolic effects. The compound is administered by appropriate routes, and insulin sensitivity, plasma glucose, and mitochondrial capacity are assessed. SRT1460 improves insulin sensitivity, lowers plasma glucose, and increases mitochondrial capacity in these models. Doses and administration routes are optimized based on the specific model.
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| ADME/Pharmacokinetics |
SRT1460 has a molecular formula of C26H22F3N3O3S and a molecular weight of 513.53. Its CAS number is 925432-73-1. The compound is a potent and selective activator of Sirtuin 1 (SIRT1) with an EC1.5 of 2.9 μM. It displays good selectivity for SIRT1 versus SIRT2 and SIRT3. SRT1460 is a synthetic small-molecule activator of SIRT1.
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| Toxicity/Toxicokinetics |
SRT1460 is a SIRT1 activator with a well-characterized mechanism of action. As with any sirtuin modulator, potential toxicity may include effects on metabolism and cellular function. The compound's safety profile should be evaluated in preclinical toxicology studies. SRT1460 is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying SIRT1 biology and metabolism.
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| References |
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| Additional Infomation |
SRT1460 (CAS# 925432-73-1) is a potent and selective activator of Sirtuin 1 (SIRT1) with an EC1.5 of 2.9 μM. It displays good selectivity for SIRT1 versus SIRT2 and SIRT3. SRT1460 reduces pancreatic cancer cell viability and improves insulin sensitivity and glucose homeostasis in obese mice models. The compound is for research use only and not for human therapeutic use.
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| Molecular Formula |
C26H29N5O4S
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| Molecular Weight |
507.6
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| Exact Mass |
507.194
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| CAS # |
925432-73-1
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| PubChem CID |
24180124
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.669
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| LogP |
3.88
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
36
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| Complexity |
714
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SBEWVVLMFLTQFE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H29N5O4S/c1-33-22-12-17(13-23(34-2)24(22)35-3)25(32)28-20-7-5-4-6-19(20)21-15-31-18(16-36-26(31)29-21)14-30-10-8-27-9-11-30/h4-7,12-13,15-16,27H,8-11,14H2,1-3H3,(H,28,32)
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| Chemical Name |
3,4,5-trimethoxy-N-[2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]benzamide
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| Synonyms |
SRT 1460; SRT-1460; SRT1460
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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 : ~10 mg/mL (~19.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.46 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 12.5 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: ≥ 1.25 mg/mL (2.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9701 mL | 9.8503 mL | 19.7006 mL | |
| 5 mM | 0.3940 mL | 1.9701 mL | 3.9401 mL | |
| 10 mM | 0.1970 mL | 0.9850 mL | 1.9701 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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