| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
mTOR (mammalian target of rapamycin) and AMPK (AMP-activated protein kinase). MHY-1685 is an mTOR inhibitor and an activator of the AMPK signaling pathway.
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|---|---|
| ln Vitro |
MHY-1685 is a novel mTOR inhibitor that also targets the AMPK signaling pathway. By inhibiting mTOR and activating AMPK, it promotes autophagy, which is a critical cellular process for the clearance of damaged proteins and organelles. MHY-1685 is a senescence inhibitor that can rejuvenate senile human cardiac stem cells (hCSCs) by modulating autophagy.
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| ln Vivo |
In vivo, MHY-1685 has been shown to improve hCSC-based myocardial regeneration. As an mTOR inhibitor and autophagy activator, it promotes the rejuvenation of senile cardiac stem cells, which may enhance their regenerative capacity.
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| Enzyme Assay |
In vitro enzyme assays for MHY-1685 are performed to evaluate its inhibitory activity against mTOR and its activation of AMPK. The kinases are incubated with substrates and ATP in the presence of varying concentrations of MHY-1685. The inhibition of mTOR activity and the activation of AMPK are measured, and IC50 values are calculated.
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| Cell Assay |
In vitro cell-based assays are conducted to evaluate the effects of MHY-1685 on autophagy, senescence, and cell viability. Human cardiac stem cells (hCSCs) are treated with MHY-1685, and autophagy is assessed by measuring LC3-II levels and autophagosome formation. Cellular senescence is assessed by measuring senescence-associated β-galactosidase activity and the expression of senescence markers. Cell viability and proliferation are assessed using standard assays.
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| Animal Protocol |
In vivo animal studies with MHY-1685 are conducted in models of myocardial injury or cardiac aging to evaluate its effects on cardiac regeneration. The compound is typically administered via oral or intraperitoneal routes. Its effects on cardiac function, stem cell rejuvenation, and autophagy markers are assessed.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for MHY-1685. As a small molecule inhibitor, its ADME properties would be characterized in standard preclinical studies.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for MHY-1685. As an mTOR inhibitor, its toxicity profile would be expected to be related to its mechanism of action. Standard safety assessments would be required for any therapeutic development.
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| References | |
| Additional Infomation |
MHY-1685 is a novel mTOR inhibitor and senescence inhibitor that activates autophagy through the AMPK pathway. It can rejuvenate senile human cardiac stem cells and offers opportunities to improve myocardial regeneration. The compound is a valuable research tool for studying cellular senescence, autophagy, and cardiac regeneration. It is not approved for human therapeutic use and is strictly for research purposes.
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| Molecular Formula |
C11H8N2O4
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|---|---|
| Molecular Weight |
232.19
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| Exact Mass |
232.048
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| CAS # |
27406-31-1
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| PubChem CID |
5292673
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
0.799
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
372
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C=C2C(=O)NC(=O)NC2=O)O
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| InChi Key |
KSOJQSBHVKAHPC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H8N2O4/c14-7-3-1-6(2-4-7)5-8-9(15)12-11(17)13-10(8)16/h1-5,14H,(H2,12,13,15,16,17)
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| Chemical Name |
5-[(4-hydroxyphenyl)methylidene]-1,3-diazinane-2,4,6-trione
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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: 62.5 mg/mL (269.18 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (8.96 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3068 mL | 21.5341 mL | 43.0682 mL | |
| 5 mM | 0.8614 mL | 4.3068 mL | 8.6136 mL | |
| 10 mM | 0.4307 mL | 2.1534 mL | 4.3068 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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