CMS-121 is an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor. CMS-121 protects HT22 cells against ischemia and oxidative damage with EC50 values of 7 nM and 200 nM, respectively. CMS-121 has strong neuroprotective, anti-inflammatory, antioxidative and renoprotective activities. CMS-121 can increase acetyl-CoA in cells.
In vivo, CMS-121 (~20 mg/kg; oral administration; daily; for 4 months; female SAMP8 mice) treatment reduces cognitive decline as well as metabolic and transcriptional markers of aging in the brain when administered to rapidly aging SAMP8 mice. CMS-121 preserves mitochondrial homeostasis by regulating acetyl-coenzyme A (acetyl-CoA) metabolism.
| Molecular Weight | 321.37 |
| Formula | C20H19NO3 |
| CAS Number | 1353224-53-9 |
| Solubility (25°C) | DMSO 48 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Acetyl-CoA Carboxylase Products |
|---|
| Sethoxydim
Sethoxydim is a postemergent herbicide. |
| A-908292
A-908292 is a potent and selective acetyl-CoA carboxylase 2 (ACC2) inhibitor, with an IC50 of 38 nM. A-908292 can be used for the research of fatty acid metabolism. |
| PF-05221304
PF-05221304 is an orally bioavailable, liver-targeted inhibitor of acetyl-CoA carboxylase (ACC), an enzyme that catalyzes the first step of adipogenesis ab initio (DNL). |
| MK-4074
MK-4074 is a liver-specific inhibitor of acetyl-CoA carboxylase ACC1 and ACC2 with IC50 values of approximately 3 nM. |
| Firsocostat (ND-630)
ND-630 is an ACC inhibitor of human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively. |
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