雷帕黴菌(Rapamycin)| Romidepsin (FK228, depsipeptide) | Daptomycin | G-418 (80 S 核醣體延伸抑制劑)
鹽酸二甲雙胍(Metformin HCl) | CAS#1115-70-4 APExBIO 貨號B1970 (10mM/10g/50g)
Anti-diabetic drug
鹽酸二甲雙胍(Metformin HCl) 是治療 2 型糖尿病(type 2 diabetes)最有效和廣泛使用的治療藥物之一。它選擇性地降低肝臟糖異生(hepatic gluconeogenesis)而不增加胰島素(insulin)的產生,從而導致體重增加(weight gain)或低血糖(hypoglycemia)。 [1]AMPK(5'AMP 活化蛋白激酶)充當代謝主開關(metabolic master switch),調節多個細胞內系統,包括的細胞葡萄糖攝取(cellular uptake of glucose)、脂肪酸的 β 氧化(-oxidation)以及 GLUT4(glucose transporter 4, 葡萄糖轉運蛋白 4)和粒線體(mitochondria)的生物合成。在肝細胞(hepatocytes)中,AMPK 被二甲雙胍(metformin)激活,隨後 ACC(acetyl-CoA carboxylase, 乙醯輔酶 A 羧化酶)活性降低,誘導脂肪酸氧化(fatty acid oxidization)並抑制脂肪生成酶(lipogenic enzyme expression)表達。 [2] Metformin還抑制 mGPD(mitochondrial lycerophosphate dehydrogenase, 線粒體甘油磷酸脫氫酶),一種氧化還原穿梭酶(redox shuttle enzyme),導致肝細胞氧化還原狀態改變(hepatocellular redox state)、乳酸(lactate)轉化減少和肝醣異生(hepatic gluconeogenesis)減少。 [1]在用metformin治療的大鼠中,SEREP-1 mRNA/蛋白的肝臟表達和 ACC 活性降低。 [2] 在二甲雙胍治療的小鼠中,肝臟中的 LKB1 對於metformin降低血糖的能力至關重要 [3]。在大鼠肝臟 mGOD 的 ASO(反義寡核苷酸)敲低中,表型與慢性二甲雙胍治療相似。它消除了 mefromin 誘導的細胞溶質氧化還原狀態、血漿葡萄糖濃度的降低和 EGP 抑制。 [1]
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 165.62 |
Cas No. | 1115-70-4 |
Formula | C4H12ClN5 |
Solubility | insoluble in EtOH; ≥30.7 mg/mL in H2O; ≥8.3 mg/mL in DMSO |
Chemical Name | 3-(diaminomethylidene)-1,1-dimethylguanidine;hydrochloride |
SDF | Download SDF |
Canonical SMILES | CN(C)C(=N)N=C(N)N.Cl |
Shipping Condition | Ship with blue ice, or upon other requests. |
General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
- 1. HangSun, YufengZhou, et al. "Metformin protects 5-Fu-induced chemotherapy oral mucositis by reducing endoplasmic reticulum stress in mice." Eur J Pharm Sci. 2022 Jun 1;173:106182. PMID: 35405270
- 2. Alain Aguilar-Valdes, Lilia G. Noriega, et al. "SWATH-MS proteomics of PANC-1 and MIA PaCa-2 pancreatic cancer cells allows identification of drug targets alternative to MEK and PI3K inhibition." Biochem Biophys Res Commun. 2021 Mar 16;552:23-29. PMID: 33740661
- 3. Ma W, Liang F, et al. "Activated FMS-like tyrosine kinase 3 ameliorates angiotensin II-induced cardiac remodelling." Acta Physiol (Oxf). 2020;e13519. PMID: 32480429
- 4. Yeo SK, Paul R, et al. "Improved efficacy of mitochondrial disrupting agents upon inhibition of autophagy in a mouse model of BRCA1-deficient breast cancer." Autophagy. 2018;14(7):1214-1225. PMID: 29938573
- 5. Dong L, Li Y, et al. "Dietary Apostichopus japonicus Alleviates Diabetes Symptoms and Modulates Genes Expression in Kidney Tissues of db/db Mice." J Agric Food Chem. 2018 Jan 2. PMID: 29249162
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APExBIO提供優質的勝肽和生物分析試劑,廣泛產品線如Protease、Chromatin/Epigenetics表觀遺傳學、MAPK Signal、DNA Damege/DNA repair、細胞凋亡、腫瘤生物學、Stem cell等研究領域, 還提供定制的服務,包括多肽合成,抗體的生產和檢測的發展。產品線DNA/RNA prep kit、Drug Screening panel、Bioactive peptides、Growth factors、Biotinylation Reagents、tag peptides、amino Acids、Growth factors等。APExBIO產品質量都伴隨著證書的分析,高效液相色譜,質譜,和HMNR數據。
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