【SIRT1 activator】白藜蘆醇 (Resveratrol)/SRT1720/SRT2104 (GSK2245840)
天然多酚植物抗毒素(polyphenolic phytoalexin)-白藜蘆醇 (Resveratrol)
白藜蘆醇(Resveratrol)是一種最初從藜蘆(Veratrum grandiflorum)中分離出來的酚類物質，富含於葡萄( grapes)、葡萄酒(wine)、花生、大豆( soy)和漿果(berries)中，幾十年來一直吸引著科學家和醫生的注意。許多研究報告道白藜蘆醇具有多種生物活性，如抗氧化(antioxidant)、抗發炎(anti-inflammatory)、心血管保護(cardiovascular protection)、抗癌(anticancer)、抗糖尿病(antidiabetes)、抗肥胖(antiobesity)、神經保護(neuroprotection)和抗衰老( antiaging effects)等作用。
白藜蘆醇 (Resveratrol)| CAS#501-36-0 APExBIO貨號 A4182
SIRT1 activator Purity: 99.94%
白藜蘆醇 (Resveratrol) 標準品用於研究和分析應用。白藜蘆醇(Resveratrol)（反式白藜蘆醇；SRT501）是一種天然多酚植物抗毒素(polyphenolic phytoalexin)，具有抗氧化(anti-oxidant)、抗發炎(anti-inflammatory)、心臟保護(cardioprotective)和抗癌特性(anti-cancer properties)。白藜蘆醇(SRT 501) 具有廣泛的目標，包括mTOR、 JAK、 β-澱粉樣蛋白(β-amyloid)、腺苷酸環化酶(Adenylyl cyclase)、 IKKβ、 DNA 聚合酶(DNA polymerase)。白藜蘆醇(Resveratrol)也是一種特殊的SIRT1激活劑。白藜蘆醇(Resveratrol)是一種有效的孕烷 X 受體 ( potent pregnane X receptor PXR) 抑制劑。白藜蘆醇是一種Nrf2活化劑，可改善小鼠模型中與老化相關的進行性腎損傷。白藜蘆醇(Resveratrol)可增加內皮細胞中 NO 的產生。
在初代神經元培養物中，白藜蘆醇 (Resveratrol) （0.1、1 和10 μM）可抑制OGD/再灌注誘導的細胞凋亡(reperfusion-induced apoptosis)，並以濃度依賴性方式抑制caspase-3 和caspase-12 mRNA 的過度表達。在神經母細胞瘤 SH-SY5Y 細胞株中，白藜蘆醇 (50 μM) 透過改善細胞內氧化壓力( oxidative stress )和增加促存活基因 Bcl-2 (prosurvival gene Bcl-2)的活性來抑制過量多巴胺(dopamine-induced cell death )誘導的細胞死亡。在遭受心肌缺血(myocardial ischemia)的大鼠中，白藜蘆醇 (Resveratrol)（2.5、5.0 mg/kg）透過改善缺血後心室恢復、減少心肌梗塞面積(myocardial infarct size)和心肌細胞凋亡來表現出心臟保護作用。然而，25 或 50 mg/kg 劑量的白藜蘆醇會抑制心臟功能，並增加心肌梗塞面積(myocardial infarct size)和凋亡細胞數量。
- 1. Xin Chou, Xiaohu Li, et al. “Sirtuin-1 attenuates cadmium-induced renal cell senescence through p53 deacetylation.” Ecotoxicol Environ Saf. 2022 Oct 15;245:114098. PMID: 36137422
- 2. Li Y, Xi Y, et al. “Sirtuin 1 activation alleviates primary biliary cholangitis via the blocking of the NF-κB signaling pathway.” Int Immunopharmacol. 2020;83:106386. PMID: 32193100
- 3. Song Y, Chen Y, et al. “Resveratrol Suppresses Epithelial-Mesenchymal Transition in GBM by Regulating Smad-Dependent Signaling.” Biomed Res Int. 2019 Apr 7;2019:1321973. PMID: 31119150
- 4. Chou X, Ding F, et al. “Sirtuin-1 ameliorates cadmium-induced endoplasmic reticulum stress and pyroptosis through XBP-1s deacetylation in human renal tubular epithelial cells.” Arch Toxicol. 2019 Feb 22. PMID: 30796460
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 228.24 |
| Cas No. | 501-36-0 |
| Formula | C14H12O3 |
| Solubility | insoluble in H2O; ≥48.2 mg/mL in EtOH with ultrasonic; ≥9.65 mg/mL in DMSO |
| Chemical Name | 5-[(E)-2-(4-hydroxyphenyl)ethenyl]benzene-1,3-diol |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=CC=C1C=CC2=CC(=CC(=C2)O)O)O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
SIRT1 活化劑(SIRT1 activator)-SRT1720
SRT1720 HCl| CAS#1001645-58-4 APExBIO貨號 A4180
SIRT1 activator Purity: 99.52%
SRT1720是一種小分子化合物( small-molecule compound)，能夠在體外活化sirtuin亞型SIRT1。 SRT1720 作為 SIRT1 活化劑(SIRT1 activator)的活性比白藜蘆醇(resveratrol)更強。它以 Sirt1 和 PGC-1α 依賴性方式影響粒線體呼吸(mitochondrial respiration)。 SRT1720 已被證明可以增強胰島素敏感性( insulin sensitivity)並改善粒線體能力(mitochondrial capacity)和氧化代謝(oxidative metabolism)。使用 SRT1720 治療多發性骨髓瘤 (multiple myeloma, MM) 細胞，可抑制對傳統療法和硼替佐米療法(bortezomib therapies )抗藥性的 MM 細胞的生長並誘導細胞凋亡，而不會顯著影響正常細胞的活力。 SRT1720 能夠增強硼替佐米(bortezomib)或地塞米鬆(dexamethasone)的細胞毒性活性(cytotoxic activity )。 SRT1720的抗MM活性與：1) caspase-8、caspase-9、caspase-3、聚(ADP)核糖聚合酶的活化； 2）活性氧(reactive oxygen species)增加； 3) 誘導磷酸化共濟失調毛細血管擴張突變(phosphorylated ataxia telangiectasia mutated)/檢查點激酶2訊號傳導； 4) 血管內皮生長因子誘導的MM細胞遷移及相關血管新生減少； 5) 抑制核因子-κB。SRT1720 是一種 SIRT1 活化劑。與對照組相比，它使 VEGF 濃度增加了約 30%，表明 SRT1720 可能促進腫瘤的血管生成(angiogenesis of tumors)。SRT1720 並沒有顯著影響原發腫瘤的大小和重量，但使肺轉移急劇增加約 150%。
- 1. Jinan Elayyan, Idan Carmon, et al. “Lef1 ablation alleviates cartilage mineralization following posttraumatic osteoarthritis induction.” Proc Natl Acad Sci U S A. 2022 May 24;119(21):e2116855119. PMID: 35594394
- 2. Xueyu Hu, Gangning Feng, et al. “The Protective Mechanism of SIRT1 on Cartilage Through Regulation of LEF-1.” Research Square. doi.org/10.21203/rs.3.rs-214497/v1.
- 3. Yangyang Li, Lei Wang, et al. “SIRT1 Mediates Neuropathic Pain Induced by Sciatic Nerve Chronic Constrictive Injury in the VTA-NAc Pathway.” Pain Res Manag 2020 Aug 18;2020:4245968. PMID: 32922581
- 4. Li Y, Xi Y, et al. “Sirtuin 1 activation alleviates primary biliary cholangitis via the blocking of the NF-κB signaling pathway.” Int Immunopharmacol. 2020;83:106386. PMID: 32193100
- 5. Lin Y, Liu J, et al. “FADD Phosphorylation Modulates Blood Glucose Levels by Decreasing the Expression of Insulin-Degrading Enzyme.” Mol Cells. 2020;43(4):373-383. PMID: 32191993
- 6. Gao P, Li L, et al. “Activation of Transient Receptor Potential Channel Vanilloid 4 by DPP-4 (Dipeptidyl Peptidase-4) Inhibitor Vildagliptin Protects Against Diabetic Endothelial Dysfunction.” Hypertension. 2019 Nov 18:HYPERTENSIONAHA11913778. PMID: 31735085
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 506.02 |
| Cas No. | 1001645-58-4 |
| Formula | C25H23N7OS·HCl |
| Synonyms | SRT-1720,SRT 1720,SRT 1720 Hydrochloride |
| Solubility | ≥25.3 mg/mL in DMSO; insoluble in EtOH; ≥15.37 mg/mL in H2O with gentle warming and ultrasonic |
| Chemical Name | N-[2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]quinoxaline-2-carboxamide;hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | C1CN(CCN1)CC2=CSC3=NC(=CN23)C4=CC=CC=C4NC(=O)C5=NC6=CC=CC=C6N=C5.Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
SIRT1 活化劑(SIRT1 activator)-SRT2104 (GSK2245840)
SRT2104 (GSK2245840)| CAS#1093403-33-8 APExBIO貨號 A3821
SIRT1 activator,selective Purity: 98.50%
SRT2104 (GSK2245840) 是一種選擇性 SIRT1 活化劑，參與能量穩態的調節。 SIRT1，也稱為 NAD 依賴性去乙醯化酶 Sirtuin-1( NAD-dependent deacetylase sirtuin-1)，是 Sirtuin 蛋白家族的成員。體外：在以small hairpin RNA 穩定轉染以敲除 SIRT1 的 C2C12 成肌細胞中，SRT2104 增加了 AP 活性，這是成骨分化的標記。這種效果完全依賴 SIRT1 的表達 [1]。體內：在雄性C57BL/6J 小鼠中，給予SRT2104（100 mg/kg，口服）可延長標準飲食小鼠的平均壽命和最大壽命，並增強骨礦物質密度、運動協調性和胰島素敏感性，並減少發炎。短期 SRT2104 給藥可在萎縮實驗模型中保留骨骼和肌肉質量 [1]。在患有亨丁頓舞蹈症的雄性 N171-82Q HD 小鼠中，SRT2104（含 0.5% SRT2104 的飲食）有效穿透血腦障壁，減輕腦萎縮，改善運動功能，延長存活期 [2]。
| Storage | Store at -20°C |
| M.Wt | 516.64 |
| Cas No. | 1093403-33-8 |
| Formula | C26H24N6O2S2 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥6.46 mg/mL in DMSO with gentle warming |
| Chemical Name | 4-methyl-N-[2-[3-(morpholin-4-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]-2-pyridin-3-yl-1,3-thiazole-5-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(SC(=N1)C2=CN=CC=C2)C(=O)NC3=CC=CC=C3C4=CN5C(=CSC5=N4)CN6CCOCC6 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |