CAD031
Based on 1 Customer Validation
CAD031 is an orally active AMPK/ACC1 signaling pathway activator and a derivative of the Alzheimer's disease (AD) targeted agent J147 (HY-13779) (more active than J147 in human neural stem cell assays). CAD031 can cross the blood-brain barrier, activate AMPK and inhibit ACC1, thereby increasing ac-CoA levels, improving mitochondrial function and reducing free fatty acid synthesis. CAD031 has neuroprotective, neurogenesis-promoting and memory-improving activities and can be used in the study of Alzheimer's disease and aging-related neurodegenerative diseases. CAD031 effectively enhances the memory of mice, improves dendritic structure, and stimulates cell division in the germinal zone of the brain of elderly mice.
For research use only. We do not sell to patients.
- Purity : 99.39%
- CAS No.: 2071209-49-7
- Formula: C18H14F6N2O2
- Molecular Weight:404.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
CAD031 (100 nM; 7 d) significantly induces the mRNA expression of neurogenesis markers Nestin, Pax6, DCX, and Ki67 in human neural precursor cells (hNPCs) experiments; and 1 μM CAD031 inhibits Aβ-induced cell death in MC65 cells and glutamate-induced cytotoxicity in HT22 cells, exerting neuroprotective activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Human embryonic stem cell-derived neural progenitor cells (Hues6 and H9)
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Concentration:100 nM
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Incubation Time:7 days
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Result:Increased transcript levels of neurogenesis-related genes (Nestin, Pax6, DCX, Ki67) compared to control, while showing no significant effect on early stem cell markers (Sox1, Sox2). The effect was normalized to fibroblast growth factor (FGF).
In Vivo
CAD031 (200 ppm; dietary administration; daily; 4 months) extends median lifespan, maintained mitochondrial gene expression and protein levels, reduces plasma free fatty acids, and activates the hepatic AMPK/ACC1 pathway in rapidly aging SAMP8 mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:APPswe/PS1ΔE9 Transgenic AD Mouse Model** Female APPswe/PS1ΔE9 transgenic mice (3 months old, weight not specified) + wild-type (WT) C57BL/6 controls[2]
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Dosage:200 ppm (premixed in diet)
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Administration:Dietary administration, daily for 6 months
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Result:Rescued context-dependent fear memory deficits in AD mice (increased freezing time) and restored the recognition index in a spatial pattern separation test.
Increased the number of BrdU+ cells in the dentate gyrus and BrdU+/DCX+ neural progenitors in the subventricular zone, while having no effect on Aβ plaque number or size.
Chemical Information
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CAS No. 2071209-49-7
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Appearance Solid
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Molecular Weight 404.31
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Formula C18H14F6N2O2
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Color Light yellow to yellow
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SMILES
O=C(N(C1=CC=C(C)C=C1C)/N=C/C2=CC=CC(OC(F)(F)F)=C2)C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (247.33 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.18 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Mitochondrial membrane-potential fluorescent assay
Mitochondrial membrane potential fluorescent assays estimate ΔΨm in living cells using lipophilic cationic dyes such as TMRM, TMRE, rhodamine 123, and JC-1, which accumulate in mitochondria according to membrane polarization; loss of signal after FCCP or CCCP treatment is interpreted as mitochondrial depolarization. TMRM/TMRE and rhodamine 123 are commonly used for semi-quantitative live-cell microscopy or flow cytometry, while JC-1 can report a shift from red aggregate fluorescence to green monomer fluorescence during depolarization; interpretation requires controls because dye concentration, quenching mode, cell type, dye efflux, and mitochondrial mass can affect fluorescence independently of ΔΨm.
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hPSC directed neural induction/NPC culture
Directed neural induction of hPSCs uses inhibition of BMP and TGF-β/Activin/Nodal SMAD signaling to bias pluripotent cells toward neuroectoderm; the readout is emergence of neural plate/rosette-like cells and neural progenitor markers such as PAX6, SOX1/SOX2, and Nestin, followed by expandable NPCs that can generate neuronal lineages.
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Mitochondrial membrane-potential and mitochondrial mass staining
Mitochondrial membrane potential staining measures the electrochemical polarization across the mitochondrial inner membrane in live cells using lipophilic cationic fluorescent probes; early rhodamine-based work showed that selective mitochondrial dye accumulation is lost when the mitochondrial transmembrane potential is dissipated. JC-1 reports mitochondrial polarization by shifting from green monomer fluorescence to red J-aggregate fluorescence as dye concentration increases within energized mitochondria; therefore, the red/green fluorescence ratio is used as a relative readout of mitochondrial membrane potential. TMRE or TMRM staining provides a single-channel relative readout because these cationic rhodamine esters accumulate in polarized mitochondria, and lower fluorescence indicates reduced mitochondrial polarization when acquisition and dye-loading conditions are controlled. Mitochondrial mass staining is commonly performed with MitoTracker Green FM or related MitoTracker dyes as
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SH-SY5Y neuronal-like differentiation
SH-SY5Y neuronal-like differentiation uses defined culture conditions to shift proliferative human neuroblastoma cells toward a neuron-like state, mainly assessed by reduced proliferation, neurite extension, neuronal-marker expression, and, in some protocols, increased dependence on neurotrophic support. Retinoic acid (RA) is commonly used for the first differentiation phase, and sequential RA followed by brain-derived neurotrophic factor (BDNF) in serum-free medium is a well-characterized approach for generating neuron-like SH-SY5Y cultures with extensive neurite outgrowth. The primary readouts are morphology-based neurite outgrowth and marker-based confirmation using proteins such as βIII-tubulin, MAP2, GAP43, synaptophysin, NeuN, NSE, TH, or related neuronal/synaptic markers, depending on the study endpoint.
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CFSE Dye Dilution Proliferation Assay
The CFSE (carboxyfluorescein diacetate succinimidyl ester) dye dilution proliferation assay is based on the covalent labeling of intracellular proteins by a cell-permeant fluorescent dye that becomes fluorescent upon intracellular ester cleavage and then is stably retained within cells. As labeled cells divide, the dye is partitioned equally between daughter cells, resulting in a stepwise halving of fluorescence intensity that can be quantified by flow cytometry to determine the number of cell divisions undergone by each cell population. This fluorescence dilution approach enables quantitative tracking of lymphocyte proliferation at the single-cell level over multiple rounds of division. CFSE-based proliferation analysis has been widely applied to measure antigen-driven lymphocyte expansion in vitro, where discrete fluorescence peaks correspond to successive cell divisions and allow reconstruction of proliferative history within heterogeneous populations.
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Dye-dilution cell tracking and proliferation staining
Dye-dilution cell tracking assays quantify cell proliferation by covalently labeling intracellular proteins with a stable fluorescent dye that is equally partitioned between daughter cells during mitosis, resulting in stepwise halving of fluorescence intensity with each cell division as measured by flow cytometry histograms. Carboxyfluorescein diacetate succinimidyl ester (CFSE) is a prototypical dye that diffuses into cells, is enzymatically converted into a fluorescent compound, and then covalently binds intracellular amine groups, producing long-lived fluorescence suitable for tracking multiple rounds of division in vitro and in vivo. Successive generations of dividing cells form discrete peaks of decreasing fluorescence intensity, enabling estimation of proliferation history, precursor frequency, and division index within heterogeneous populations. Alternative dyes such as CellTrace Violet (CTV) and far-red membrane dyes (e. g. , PKH26) follow the same dilution principle but differ
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Cell differentiation
Cell differentiation refers to the process in which cells of the same origin gradually produce cell groups with different morphological structure and functional characteristics.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Prior M, et al. Selecting for neurogenic potential as an alternative for Alzheimer's disease drug discovery. Alzheimers Dement. 2016 Jun;12(6):678-86. [Content Brief]
[2]. Currais A, et al. A chemical biology approach to identifying molecular pathways associated with aging. Geroscience. 2021 Feb;43(1):353-365. [Content Brief]
[3]. Kepchia D, et al. The Alzheimer's disease drug candidate J147 decreases blood plasma fatty acid levels via modulation of AMPK/ACC1 signaling in the liver. Biomed Pharmacother. 2022 Mar;147:112648. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4733 mL | 12.3667 mL | 24.7335 mL | 61.8337 mL |
| 5 mM | 0.4947 mL | 2.4733 mL | 4.9467 mL | 12.3667 mL | |
| 10 mM | 0.2473 mL | 1.2367 mL | 2.4733 mL | 6.1834 mL | |
| 15 mM | 0.1649 mL | 0.8244 mL | 1.6489 mL | 4.1222 mL | |
| 20 mM | 0.1237 mL | 0.6183 mL | 1.2367 mL | 3.0917 mL | |
| 25 mM | 0.0989 mL | 0.4947 mL | 0.9893 mL | 2.4733 mL | |
| 30 mM | 0.0824 mL | 0.4122 mL | 0.8244 mL | 2.0611 mL | |
| 40 mM | 0.0618 mL | 0.3092 mL | 0.6183 mL | 1.5458 mL | |
| 50 mM | 0.0495 mL | 0.2473 mL | 0.4947 mL | 1.2367 mL | |
| 60 mM | 0.0412 mL | 0.2061 mL | 0.4122 mL | 1.0306 mL | |
| 80 mM | 0.0309 mL | 0.1546 mL | 0.3092 mL | 0.7729 mL | |
| 100 mM | 0.0247 mL | 0.1237 mL | 0.2473 mL | 0.6183 mL |
CAD031 Related Classifications
HY-124609 Related Classifications
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