CMS121 |
カタログ番号GC40632
One-Click Copy Product Info
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CMS121は経口活性のアセチル-CoAカルボキシラーゼ1 (ACC1)阻害剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1353224-53-9
Sample solution is provided at 25 µL, 10mM.
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CMS121は経口活性のアセチル-CoAカルボキシラーゼ1 (ACC1)阻害剤である[1]。CMS121は、アセチル-CoAのレベルを上昇させ、AMPKを活性化することで、有力な神経保護、抗炎症、抗酸化と腎保護作用を発揮する[2-3]。CMS121は、主にアルツハイマー様の神経変性疾患の治療に使われる[4]。
SH-SY5Y細胞で、CMS121 (5μM; 48h)はHSV-1ウイルス粒子の感染性を減らす[5]。肝細胞で、CMS12 (1μM; 24h)はac-STAT3とp-STAT3のレベルを増やす[6]。
雄のdb/dbマウスで、長期的なCMS121 (9.4mg/kg, 18.8mg/kg；経口；24週間)処理は、代謝の不均衡、肝炎症を軽減し、腎損傷のマーカーを減らす[7]。SAMP8マウスモデルで、CMS121 (17mg/kg；経口；9週間)の処理は、聴性脳幹反応閾値ドリフトを著しく減らし、中周波数域で内有毛細胞リボンシナプスの保存性を増やした[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.
| 細胞実験[1]: | |
細胞株 | SH-SY5Y細胞 |
準備方法 | CMS121の細胞毒性を測定するために、SH-SY5Y細胞を96ウェルの培養プレートに播種し、翌日に、増加する濃度の化合物、または溶媒ジメチルスルホキシド（DMSO）に暴露した。48時間の培養後、生細胞の数を、3-(4,5-ジメチルチアゾール-2-イル)-2,5-ジフェニルテトラゾリウム臭化物（MTT）アッセイで測定した。似たように、shCTRLとshFASN細胞をコンフルエンスに成長させた。その後、培地を無血清培地に交換し、48時間後、生細胞の数をMTTアッセイで測定した。 |
反応条件 | 5μM；48時間 |
アプリケーション | CMS121は、HSV-1ウイルス粒子の感染性を減らす。 |
| 動物実験 [2]: | |
動物モデル | 雄db/dbマウス |
準備方法 | 5週齢で、雄db/dbマウスと未処理の野生型（WT）マウス(C57BL/6J)には、CMS121の添加のある/なしで、標準的な齧歯類飼料を6か月間投与した。マウス（12匹/グループ）をランダムに、処理食群（db/db + CMS121）または対照群（db/db）に分けた。WTマウスをも評価し、db/db表現型を強調するための参照グループとして使った。食物摂取量は、処理の最初の17週間は平均9.4 mg/kg/日のCMS121消費量に等しく、18から24週目は平均18.8 mg/kg/日のCMS121消費量に等しかった。 |
投与形態 | 9.4mg/kg, 18.8mg/kg；経口；24週間 |
アプリケーション | 長期的なCMS121処理は、代謝の不均衡、肝炎症を軽減し、腎損傷のマーカーを減らす。 |
References: | |
| Cas No. | 1353224-53-9 | SDF | |
| Chemical Name | 4-[4-(cyclopentyloxy)-2-quinolinyl]-1,2-benzenediol | ||
| Canonical SMILES | OC1=CC(C2=NC(C=CC=C3)=C3C(OC4CCCC4)=C2)=CC=C1O | ||
| Formula | C20H19NO3 | M.Wt | 321.4 |
| 溶解度 | 20mg/mL in DMSO, 30mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1114 mL | 15.5569 mL | 31.1139 mL |
| 5 mM | 622.3 μL | 3.1114 mL | 6.2228 mL |
| 10 mM | 311.1 μL | 1.5557 mL | 3.1114 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)