CMS121
目录号 : GC40632CMS121是一种口服有效的乙酰辅酶A羧化酶1（ACC1）抑制剂。
Cas No.:1353224-53-9
Sample solution is provided at 25 µL, 10mM.
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CMS121 is an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor [1]. CMS121 exerts potent neuroprotective, anti-inflammatory, antioxidant, and renal protective effects by elevating acetyl-CoA levels and activating AMPK [2-3]. CMS121 is primarily intended for the treatment of Alzheimer's-like neurodegenerative disorders [4].
In SH-SY5Y cells, CMS121 (5μM; 48h) reduces the infectivity of HSV-1 viral particles [5]. In hepatocytes, CMS12 (1μM; 24h) increases ac-STAT3 and p-STAT3 levels [6].
In male db/db mice, long-term CMS121 (9.4mg/kg, 18.8mg/kg; po; 24 weeks) treatment alleviates metabolic imbalance, liver inflammation, and reduces markers of kidney injury [7]. In SAMP8 mice model, treated with CMS121 (17mg/kg; po; 9 weeks) showed significantly reduced auditory brainstem responses threshold drift and increased preservation of inner hair cell ribbon synapses in the mid-frequency range [8].
References:
[1]. Dafre A L, Zahid S, Probst J J, et al. CMS121: a novel approach to mitigate aging-related obesity and metabolic dysfunction[J]. Aging (Albany NY), 2024, 16(6): 4980.
[2]. Dong J, Li M, Peng R, et al. ACACA reduces lipid accumulation through dual regulation of lipid metabolism and mitochondrial function via AMPK-PPARα-CPT1A axis[J]. Journal of Translational Medicine, 2024, 22(1): 196.
[3]. Currais A, Huang L, Petrascheck M, et al. A chemical biology approach to identifying molecular pathways associated with aging[J]. GeroScience, 2021, 43(1): 353-365.
[4]. Currais A, Raschke W, Maher P. CMS121, a novel drug candidate for the treatment of Alzheimer’s disease and age-related dementia[J]. Journal of Alzheimer’s Disease, 2024, 101(s1): S179-S192.
[5]. Albano C, Trifirò L, Hewelt-Belka W, et al. The impact of fatty acid synthase on HSV-1 infection dynamics[J]. PLoS pathogens, 2025, 21(5): e1013068.
[6]. He Y, Wang S, Liu S, et al. MSL1 promotes liver regeneration by driving phase separation of STAT3 and histone h4 and enhancing their acetylation[J]. Advanced Science, 2023, 10(23): 2301094.
[7]. Zahid S, Dafre A L, Currais A, et al. The geroprotective drug candidate CMS121 alleviates diabetes, liver inflammation, and renal damage in db/db leptin receptor deficient mice[J]. International Journal of Molecular Sciences, 2023, 24(7): 6828.
[8]. Pham T B, Boussaty E C, Currais A, et al. Attenuation of age-related hearing impairment in senescence-accelerated mouse prone 8 (SAMP8) mice treated with fatty acid synthase inhibitor CMS121[J]. Journal of Molecular Neuroscience, 2023, 73(4): 307-315.
CMS121是一种口服有效的乙酰辅酶A羧化酶1（ACC1）抑制剂 [1]。CMS121通过提高乙酰辅酶A水平和激活AMPK，发挥强大的神经保护、抗炎、抗氧化和肾脏保护作用 [2-3]。CMS121主要用于治疗阿尔茨海默病样神经退行性疾病 [4]。
在SH-SY5Y细胞中，CMS121（5μM；48h）可降低HSV-1病毒颗粒的传染性 [5]。在肝细胞中，CMS12（1μM；24h）可提高ac-STAT3和p-STAT3水平 [6]。
在雄性db/db小鼠中，长期CMS121（9.4mg/kg，18.8mg/kg；po；24周）治疗可缓解代谢失衡、肝脏炎症，并降低肾损伤标志物 [7]。在SAMP8小鼠模型中，用CMS121（17mg/kg；po；9周）治疗后，听觉脑干反应阈值漂移明显降低，中频范围内内毛细胞带状突触的保存增加 [8]。
| Cell experiment [1]: | |
Cell lines | SH-SY5Y cells |
Preparation Method | To determine the cytotoxicity of CMS121, SH-SY5Y cells were seeded in a 96-well culture plate and exposed to increasing concentrations of either compounds or vehicle dimethyl sulfoxide (DMSO) the following day. After 48h of incubation, the number of viable cells was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Similarly, shCTRL and shFASN cells were grown to confluence. The medium was then replaced with serum-free medium, and after 48 hours, the number of viable cells was measured using the MTT assay. |
Reaction Conditions | 5μM; 48h |
Applications | CMS121 reduces the infectivity of HSV-1 viral particles. |
| Animal experiment [2]: | |
Animal models | Male db/db mice |
Preparation Method | At 5 weeks of age, male db/db mice and untreated wild-type (WT) mice (C57BL/6J) were fed a standard rodent diet for 6 months with or without the addition of CMS121. Mice (12 per group) were randomly assigned to a treatment diet group (db/db + CMS121) or a control group (db/db). WT mice were also evaluated and used as a reference group to highlight the db/db phenotype. Food intake corresponded to an average consumption of 9.4mg/kg/day CMS121 during the first 17 weeks of treatment and an average consumption of 18.8mg/kg/day CMS121 during weeks 18-24. |
Dosage form | 9.4mg/kg, 18.8mg/kg; po; 24 weeks |
Applications | Long-term CMS121 treatment alleviates metabolic imbalance, liver inflammation, and reduces markers of kidney injury. |
References: | |
| Cas No. | 1353224-53-9 | SDF | |
| 化学名 | 4-[4-(cyclopentyloxy)-2-quinolinyl]-1,2-benzenediol | ||
| Canonical SMILES | OC1=CC(C2=NC(C=CC=C3)=C3C(OC4CCCC4)=C2)=CC=C1O | ||
| 分子式 | C20H19NO3 | 分子量 | 321.4 |
| 溶解度 | 20mg/mL in DMSO, 30mg/mL in DMF | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1114 mL | 15.5569 mL | 31.1139 mL |
| 5 mM | 0.6223 mL | 3.1114 mL | 6.2228 mL |
| 10 mM | 0.3111 mL | 1.5557 mL | 3.1114 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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