別品名 |
Dimethylbiguanide hydrochloride, Imidodicaronimidic diamide, N,N-dimethyl-, monohydrochloride, N,N-Dimethylbiguanide hydrochloride, 1,1-Dimethylbiguanide Hydrochloride
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別包装 |
あり
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純度 |
>=98%
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分子量 |
165.62
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CAS RN® |
1115-70-4
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化合物の概要 |
AMPK activator.
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構造 |
C4H11N5 HCl
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溶媒 |
100 mM water, 50 mM DMSO
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使用目的 |
Metformin is an AMPK activator that exhibits anti-diabetic, antihyperglycemic, antioxidative, immunosuppressive, anticancer chemotherapeutic, anti-metastatic, and chemopreventive activities. Metformin modulates glucose-6-phosphatase activity, decreasing glucose production and glycogenolysis. Additionally, it inhibits expression of TNF-α in the liver, reversing pathology of fatty liver disease in vivo. In podocytes, metformin decreases activity of NADPH oxidase and generation of free radicals. In other in vitro models, metformin inhibits expression of MHC molecules and co-stimulatory factors on dendritic cells, preventing antigen presentation. Across several hepatocellular carcinoma cell lines, metformin decreases expression of cyclin D1, cyclin E, and CDK4, inducing G0/G1 phase cell cycle arrest and inhibiting cell proliferation. In vivo, this compound also downregulates expression of c-myc, preventing neoplasia initiation in prostate cancer models. Metformin’s activation of AMPK also inhibits Shh signaling in breast cancer models, suppressing proliferation, migration, and invasion.
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その他 |
[融点]223-226
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参考文献 |
Fan C, Wang Y, Liu Z, et al. Metformin exerts anticancer effects through the inhibition of the Sonic hedgehog signaling pathway in breast cancer. Int J Mol Med. 2015 May 21. [Epub ahead of print]. PMID: 25999130.Miyoshi H, Kato K, Iwama H, et al. Effect of the anti-diabetic drug metformin in hepatocellular carcinoma in vitro and in vivo. Int J Oncol. 2013 Dec 30. [Epub ahead of print]. PMID: 24378856.Piwkowska A, Rogacka D, Jankowski M, et al. Metformin reduces NAD(P)H oxidase activity in mouse cultured podocytes through purinergic dependent mechanism by increasing extracellular ATP concentration. Acta Biochim Pol. 2013;60(4):607-12. PMID: 24432311.Akinyeke T, Matsumura S, Wang X, et al. Metformin targets c-MYC oncogene to prevent prostate cancer. Carcinogenesis. 2013 Dec;34(12):2823-32. PMID: 24130167.Zhang Y, Guan M, Zheng Z, et al. Effects of metformin on CD133+ colorectal cancer cells in diabetic patients. PLoS One. 2013 Nov 21;8(11):e81264. PMID: 24278407.Shin S, Hyun B, Lee A, et al. Metformin Suppresses MHC-Restricted Antigen Presentation by Inhibiting Co-Stimulatory Factors and MHC Molecules in APCs. Biomol Ther (Seoul). 2013 Jan;21(1):35-41. PMID: 24009856.Chu CA, Wiernsperger N, Muscato N, et al. The acute effect of metformin on glucose production in the conscious dog is primarily attributable to inhibition of glycogenolysis. Metabolism. 2000 Dec;49(12):1619-26. PMID: 11145127.Lin HZ, Yang SQ, Chuckaree C, et al. Metformin reverses fatty liver disease in obese, leptin-deficient mice. Nat Med. 2000 Sep;6(9):998-1003. PMID: 10973319.Minassian C, Tarpin S, Mithieux G. Role of glucose-6 phosphatase, glucokinase, and glucose-6 phosphate in liver insulin resistance and its correction by metformin. Biochem Pharmacol. 1998 Apr 15;55(8):1213-9. PMID: 9719475.Stumvoll M, Nurjhan N, Perriello G, et al. Metabolic effects of metformin in non-insulin-dependent diabetes mellitus. N Engl J Med. 1995 Aug 31;333(9):550-4. PMID: 7623903.Nakamichi N, Shima H, Asano S, et al. Involvement of carnitine/organic cation transporter OCTN1/SLC22A4 in gastrointestinal absorption of metformin. J Pharm Sci. 2013 Sep;102(9):3407-3417. PMID: 23666872.
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メーカー |
品番 |
包装 |
LKT
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M2076
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100 G
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※表示価格について
当社在庫 |
なし
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納期目安 |
1週間程度
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保存温度 |
常温
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