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Purity: ≥98%
CMS-121 (CMS121) is a novel and potent fisetin-based quinolone derivative acting as an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor with anti-aging, neuroprotective, anti-inflammatory, antioxidative, and renoprotective activities. It is currently in the animal toxicology studies required for FDA approval to start clinical trials for AD treatment.
| Targets |
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| ln Vitro |
ACC1 is phosphorylated at serine 79 more when treated with CMS-121 (1 µM; 4 hours; HT22 cells). Elevating acetyl-CoA in cells is possible with CMS-121 [1].
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| ln Vivo |
When given to rapidly aging SAMP8 mice, CMS-121 (~20 mg/kg; oral dose; daily; for 4 months; female SAMP8 mice) lowers both cognitive decline and metabolic and transcriptional indicators of aging in the brain. Through controlling the metabolism of acetyl-coenzyme A (acetyl-CoA), CMS-121 maintains mitochondrial homeostasis[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HT22 cells Tested Concentrations: 1 µM Incubation Duration: 4 hrs (hours) Experimental Results: Increases the phosphorylation of ACC1 at serine 79. |
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| Animal Protocol |
Animal/Disease Models: Female SAMP8 mice (9 months old)[1]
Doses: ~20 mg/kg/day Route of Administration: Oral administration; daily; for 4 months Experimental Results: decreased cognitive decline as well as metabolic and transcriptional markers of aging in the brain. |
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| References |
[1]. Currais A, et al. Elevating acetyl-CoA levels reduces aspects of brain aging. Elife. 2019 Nov 19;8. pii: e47866.
[2]. Chiruta C, et al. Chemical modification of the multitarget neuroprotective compound fisetin. J Med Chem. 2012 Jan 12;55(1):378-89. [3]. Prior M, et al. Back to the future with phenotypic screening. ACS Chem Neurosci. 2014 Jul 16;5(7):503-13. |
| Molecular Formula |
C20H19NO3
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|---|---|
| Molecular Weight |
321.369765520096
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| CAS # |
1353224-53-9
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| SMILES |
OC1=CC=C(C2=NC3=CC=CC=C3C(OC4CCCC4)=C2)C=C1O
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| InChi Key |
OMHNVUCFPJJLKD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H19NO3/c22-18-10-9-13(11-19(18)23)17-12-20(24-14-5-1-2-6-14)15-7-3-4-8-16(15)21-17/h3-4,7-12,14,22-23H,1-2,5-6H2
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| Chemical Name |
4-(4-(cyclopentyloxy)quinolin-2-yl)benzene-1,2-diol
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| Synonyms |
CMS-121, CMS 121, CMS121
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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 : ~50 mg/mL (~155.58 mM)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1117 mL | 15.5584 mL | 31.1168 mL | |
| 5 mM | 0.6223 mL | 3.1117 mL | 6.2234 mL | |
| 10 mM | 0.3112 mL | 1.5558 mL | 3.1117 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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