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伏格列波糖

α-葡萄糖苷酶抑制剂
规格或纯度: 98%
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药物成分

基本描述

规格或纯度 98%
英文名称 Voglibose
别名 伏格列波糖
英文别名 3,4-Dideoxy-4-{[2-hydroxy-1-(hydroxymethyl)ethyl]amino]-2-D-epi-inositol N-(1,3-Dihydroxyprop-2-yl)valiolamine;3,4-Dideoxy-4-{2-hydroxy-1-(hydroxymethyl)ethylamino-2-D-epi-inositol, N-(1,3-Dihydroxyprop-2-yl)valiolamine
生化机理 口服有效α-葡萄糖苷酶抑制剂(蔗糖酶和麦芽糖酶的IC50值分别为3.9和6.4 nM)。在Wistar肥胖大鼠中增加胰高血糖素样肽1(GLP-1)的分泌并减少食物摄入量,并降低血浆葡萄糖,甘油三酸酯和胰岛素的浓度。在体内表现出抗糖尿病和抗肥胖活性。
应用 伏格列波糖是一种α-葡萄糖苷酶抑制剂,与阿卡波糖(acarbose),米格列醇(miglitol)类似,用于降低糖尿病人餐后高血糖(PPHG)。伏格列波糖是用来作为胰高血糖素样肽受体和磷酸肌醇3 - 激酶Akt内皮型一氧化氮合酶路径对缺血再灌注损伤的一种保护剂.
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍

伏格列波糖是一种α-葡萄糖苷酶抑制剂,与阿卡波糖(acarbose),米格列醇(miglitol)类似,用于降低糖尿病人餐后高血糖(PPHG)。伏格列波糖是用来作为胰高血糖素样肽受体和磷酸肌醇3 - 激酶Akt内皮型一氧化氮合酶路径对缺血再灌注损伤的一种保护剂.

Voglibose is an α-glucosidase inhibitor, similar to acarbose and miglitol, used for lowering post-prandial hyperglycemia (PPHG) in people with diabetes mellitus. Voglibose is used to study it benefits as a protectant against ischemia-reperfusion injury through glucagon-like peptide 1 receptors and the phosphoinositide 3-kinase-Akt-endothelial nitric oxide synthase pathway.
Voglibose is an α-glucosidase inhibitor, similar to acarbose and miglitol, used for lowering post-prandial hyperglycemia (PPHG) in people with diabetes mellitus. Voglibose is used to study it benefits as a protectant against ischemia-reperfusion injury through glucagon-like peptide receptors and the phosphoinositide 3-kinase-Akt-endothelial nitric oxide synthase pathway.

名称和标识符

IUPAC Name (1S,2S,3R,4S,5S)-5-(1,3-dihydroxypropan-2-ylamino)-1-(hydroxymethyl)cyclohexane-1,2,3,4-tetrol
INCHI InChI=1S/C10H21NO7/c12-2-5(3-13)11-6-1-10(18,4-14)9(17)8(16)7(6)15/h5-9,11-18H,1-4H2/t6-,7-,8+,9-,10-/m0/s1
InChi Key FZNCGRZWXLXZSZ-CIQUZCHMSA-N
Canonical SMILES C1C(C(C(C(C1(CO)O)O)O)O)NC(CO)CO
分子式

C10H21NO7

PubChem CID 444020
分子量 267.28

化学和物理性质

溶解性 溶于water, 最高浓度 (mg/mL): 26.73, 最高浓度(mM): 100;溶于DMSO, 最高浓度 (mg/mL): 20.05, 最高浓度(mM): 75
敏感性 对热敏感
熔点 165°C
比旋光度 46°(C=1,0.1mol/L HCL)

安全信息

WGK Germany 3
RTECS NM7524600
Reaxy-Rn 5430708
Merck Index 10029

参考文献

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2. Jiro Nakamura.  (2005-03-23)  [Effects of voglibose, alpha-glucosidase inhibitor in treatment of impaired glucose tolerance]..  Nihon rinsho. Japanese journal of clinical medicine,  63 Suppl 2  ():  (457-461).  [PMID:15779422]
3. Ryuzo Kawamori.  (2010-05-08)  [Voglibose for the prevention of type 2 diabetes mellitus: a randomised, double-blind trial in Japanese subjects with impaired glucose tolerance]..  Nihon rinsho. Japanese journal of clinical medicine,  68  ((5)):  (873-881).  [PMID:20446586]
4. Y Iwamoto,A Kashiwagi,N Yamada,S Terao,N Mimori,M Suzuki,H Tachibana.  (2010-07-02)  Efficacy and safety of vildagliptin and voglibose in Japanese patients with type 2 diabetes: a 12-week, randomized, double-blind, active-controlled study..  Diabetes, obesity & metabolism,  12  ((8)):  (700-708).  [PMID:20590747]
5. Yasuhiro Shimojima,Wataru Ishii,Masayuki Matsuda,Kana Tojo,Rie Watanabe,Shu-Ichi Ikeda.  (2011-01-18)  Pneumatosis cystoides intestinalis in neuropsychiatric systemic lupus erythematosus with diabetes mellitus: case report and literature review..  Modern rheumatology,  21  ((4)):  (415-419).  [PMID:21240619]
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7. Michio Shimabukuro,Hiroaki Masuzaki,Masataka Sata.  (2012-02-02)  Intensive glucose lowering in cardiovascular risk management - unsolved questions - ..  Circulation journal : official journal of the Japanese Circulation Society,  76  ((3)):  (593-595).  [PMID:22293455]
8. Devasier Bennet,Mohana Marimuthu,Sanghyo Kim,Jeongho An.  (2012-08-14)  Dual drug-loaded nanoparticles on self-integrated scaffold for controlled delivery..  International journal of nanomedicine,  ():  (3399-3419).  [PMID:22888222]
9. Masahiro Inoue.  (2012-09-22)  Tighter control of postprandial hyperglycemia with mitiglinide/voglibose fixed-dose combination in Japanese patients with type 2 diabetes mellitus..  Expert opinion on pharmacotherapy,  13  ((16)):  (2257-2268).  [PMID:22994875]
10. E Araki,R Kawamori,N Inagaki,H Watada,N Hayashi,Y Horie,A Sarashina,S Thiemann,M von Eynatten,K Dugi,H-J Woerle.  (2012-11-21)  Long-term safety of linagliptin monotherapy in Japanese patients with type 2 diabetes..  Diabetes, obesity & metabolism,  15  ((4)):  (364-371).  [PMID:23163910]
11. Yuri Ono,Hiraku Kameda,Kyu Yong Cho.  (2013-02-19)  Mitiglinide/voglibose fixed-dose combination improves postprandial glycemic excursions in Japanese patients with type 2 diabetes mellitus..  Expert opinion on pharmacotherapy,  14  ((4)):  (361-370).  [PMID:23414242]
12. Chiaki Seo,Masaya Sakamoto,Rimei Nishimura,Daisuke Tsujino,Kiyotaka Ando,Aya Morimoto,Kazunori Utsunomiya.  (2013-05-03)  Comparison of glycemic variability in patients with type 2 diabetes given sitagliptin or voglibose: a continuous glucose monitoring-based pilot study..  Diabetes technology & therapeutics,  15  ((5)):  (378-385).  [PMID:23634671]
13. Bum-Ho Bin,Juyeon Seo,Seung Ha Yang,Eunkyung Lee,Hyunjung Choi,Kyu-Han Kim,Eun-Gyung Cho,Tae Ryong Lee.  (2013-07-25)  Novel inhibitory effect of the antidiabetic drug voglibose on melanogenesis..  Experimental dermatology,  22  ((8)):  (541-546).  [PMID:23879813]
14. Hyun Ju Do,Taeon Jin,Ji Hyung Chung,Ji Won Hwang,Min-Jeong Shin.  (2014-01-07)  Voglibose administration regulates body weight and energy intake in high fat-induced obese mice..  Biochemical and biophysical research communications,  443  ((3)):  (1110-1117).  [PMID:24388987]
15. Chikoto Hashiguchi,Shin-ichiro Kawamoto,Takayuki Kasai,Yasuhiro Nishi,Eiichi Nagaoka.  (2014-05-23)  Influence of an antidiabetic drug on biomechanical and histological parameters around implants in type 2 diabetic rats..  Implant dentistry,  23  ((3)):  (264-269).  [PMID:24844386]
16. Toshiyuki Takasu,Yuka Hayashizaki,Atsuo Tahara,Eiji Kurosaki,Shoji Takakura.  (2014-10-15)  Antihyperglycemic effect of ipragliflozin, a sodium-glucose co-transporter\xa02 inhibitor, in combination with oral antidiabetic drugs in mice..  Clinical and experimental pharmacology & physiology,  42  ((1)):  (87-93).  [PMID:25311502]
17. Hyang-Ki Choi,Minkyung Oh,Eun Ji Kim,Geun Seog Song,Jong-Lyul Ghim,Ji-Hong Shon,Ho-Sook Kim,Jae-Gook Shin.  (2014-12-30)  Pharmacokinetic study of metformin to compare voglibose/metformin fixed-dose combination with coadministered voglibose and metformin..  International journal of clinical pharmacology and therapeutics,  53  ((2)):  (147-153).  [PMID:25546164]
18. Hiroki Oe,Kazufumi Nakamura,Hajime Kihara,Kenei Shimada,Shota Fukuda,Tsutomu Takagi,Toru Miyoshi,Kumiko Hirata,Junichi Yoshikawa,Hiroshi Ito.  (2015-06-19)  Comparison of effects of sitagliptin and voglibose on left ventricular diastolic dysfunction in patients with type 2 diabetes: results of the 3D trial..  Cardiovascular diabetology,  14  ():  (83-83).  [PMID:26084668]
19. Atsuo Tahara,Toshiyuki Takasu,Masanori Yokono,Masakazu Imamura,Eiji Kurosaki.  (2015-10-10)  Effects of the combination of SGLT2 selective inhibitor ipragliflozin and various antidiabetic drugs in type 2 diabetic mice..  Archives of pharmacal research,  39  ((2)):  (259-270).  [PMID:26450351]
20. Kenji Akahane,Kazuma Ojima,Ayaka Yokoyama,Toshihiro Inoue,Sumiyoshi Kiguchi,Satoshi Tatemichi,Hiroo Takeda,Yohsuke Imai.  (2017-07-27)  Effects of combination of mitiglinide with various oral antidiabetic drugs in streptozotocin-nicotinamide-induced type 2 diabetic rats and Zucker fatty rats..  Clinical and experimental pharmacology & physiology,  44  ((12)):  (1263-1271).  [PMID:28744906]
21. Xiaodan Liu,Jianan Feng,Yan Li.  (2018-03-05)  Preparation of carbon-functionalized magnetic graphene/mesoporous silica composites for selective extraction of miglitol and voglibose in rat plasma..  Talanta,  182  ():  (405-413).  [PMID:29501171]
22. Kemin Tan,Christine Tesar,Rosemarie Wilton,Robert P Jedrzejczak,Andrzej Joachimiak.  (2018-05-16)  Interaction of antidiabetic α-glucosidase inhibitors and gut bacteria α-glucosidase..  Protein science : a publication of the Protein Society,  27  ((8)):  (1498-1508).  [PMID:29761590]
23. R M Coleman,G Ojeda-Torres,W Bragg,D Fearey,P McKinney,L Castrodale,D Verbrugge,K Stryker,E DeHart,M Cooper,E Hamelin,J Thomas,R C Johnson.  (2018-05-26)  Saxitoxin Exposure Confirmed by Human Urine and Food Analysis..  Journal of analytical toxicology,  42  ((7)):  (e61-e64).  [PMID:29800291]
24. Atsuo Tahara,Yoshinori Kondo,Toshiyuki Takasu,Hiroshi Tomiyama.  (2018-07-20)  Effects of the SGLT2 inhibitor ipragliflozin on food intake, appetite-regulating hormones, and arteriovenous differences in postprandial glucose levels in type 2 diabetic rats..  Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie,  105  ():  (1033-1041).  [PMID:30021338]
25. Zhi Xiang Ng,Nureen Farhana Rosman.  (2019-03-25)  In vitro digestion and domestic cooking improved the total antioxidant activity and carbohydrate-digestive enzymes inhibitory potential of selected edible mushrooms..  Journal of food science and technology,  56  ((2)):  (865-877).  [PMID:30906044]
26. Mai Sotoyama,Shinya Uchida,Chiaki Kamiya,Shimako Tanaka,Yasuharu Kashiwagura,Akio Hakamata,Keiichi Odagiri,Naoki Inui,Hiroshi Watanabe,Noriyuki Namiki.  (2019-06-04)  Ease of Taking and Palatability of Fixed-Dose Orally Disintegrating Mitiglinide/Voglibose Tablets..  Chemical & pharmaceutical bulletin,  67  ((6)):  (540-545).  [PMID:31155559]
27. Shipra Bhansali,Anil Bhansali,Pinaki Dutta,Rama Walia,Veena Dhawan.  (2020-01-25)  Metformin upregulates mitophagy in patients with T2DM: A randomized placebo-controlled study..  Journal of cellular and molecular medicine,  24  ((5)):  (2832-2846).  [PMID:31975558]
28. Junichi Kato,Yohei Shirakami,Taku Mizutani,Masaya Kubota,Hiroyasu Sakai,Takashi Ibuka,Masahito Shimizu.  (2020-03-27)  Alpha-Glucosidase Inhibitor Voglibose Suppresses Azoxymethane-Induced Colonic Preneoplastic Lesions in Diabetic and Obese Mice..  International journal of molecular sciences,  21  ((6)):  ().  [PMID:32210144]
29. Xiaolong Chen,Yuguo Zheng,Yinchu Shen.  (2006-02-07)  Voglibose (Basen, AO-128), one of the most important alpha-glucosidase inhibitors..  Current medicinal chemistry,  13  ((1)):  (109-116).  [PMID:16457643]
30. Makoto Hiki,Kazunori Shimada,Takashi Kiyanagi,Kosuke Fukao,Kuniaki Hirose,Hiromichi Ohsaka,Yoshifumi Fukushima,Atsumi Kume,Rie Matsumori,Katsuhiko Sumiyoshi,Tetsuro Miyazaki,Hirotoshi Ohmura,Takeshi Kurata,Takashi Miida,Hiroyuki Daida.  (2010-06-04)  Single administration of alpha-glucosidase inhibitors on endothelial function and incretin secretion in diabetic patients with coronary artery disease - Juntendo University trial: effects of miglitol on endothelial vascular reactivity in type 2 diabetic patients with coronary heart disease (J-MACH) -..  Circulation journal : official journal of the Japanese Circulation Society,  74  ((7)):  (1471-1478).  [PMID:20519875]
31. Y Iwamoto,N Tajima,T Kadowaki,K Nonaka,T Taniguchi,M Nishii,J C Arjona Ferreira,J M Amatruda.  (2010-07-02)  Efficacy and safety of sitagliptin monotherapy compared with voglibose in Japanese patients with type 2 diabetes: a randomized, double-blind trial..  Diabetes, obesity & metabolism,  12  ((7)):  (613-622).  [PMID:20590736]
32. Xiu-mei Dai,Ning An,Jian-min Wu,Hui-yi Li,Qi-ming Zhang.  (2011-02-26)  Development and validation of HPLC-UV-MS method for the control of four anti-diabetic drugs in suspected counterfeit products..  Yao xue xue bao = Acta pharmaceutica Sinica,  45  ((3)):  (347-352).  [PMID:21348424]
33. Keisuke Fujitaka,Hajime Otani,Fusakazu Jo,Hiromi Jo,Emiko Nomura,Masayoshi Iwasaki,Mitsushige Nishikawa,Toshiji Iwasaka.  (2011-04-19)  Comparison of metabolic profile and adiponectin level with pioglitazone versus voglibose in patients with type-2 diabetes mellitus associated with metabolic syndrome..  Endocrine journal,  58  ((6)):  (425-432).  [PMID:21498915]
34. Ryuzo Kawamori.  (2011-07-20)  [Evidence demonstrating the effect of voglibose for the prevention of type 2 diabetes mellitus: a randomised double-blind trial in Japanese subjects with inpaired glucose tolerance]..  Nihon rinsho. Japanese journal of clinical medicine,  69 Suppl 1  ():  (663-670).  [PMID:21766678]
35. T Narita,H Yokoyama,R Yamashita,T Sato,M Hosoba,T Morii,H Fujita,K Tsukiyama,Y Yamada.  (2011-11-05)  Comparisons of the effects of 12-week administration of miglitol and voglibose on the responses of plasma incretins after a mixed meal in Japanese type 2 diabetic patients..  Diabetes, obesity & metabolism,  14  ((3)):  (283-287).  [PMID:22051162]
36. Yu Kataoka,Satoshi Yasuda,Yoshihiro Miyamoto,Kazuhiro Sase,Masami Kosuge,Kazuo Kimura,Yasunao Yoshimasa,Shunichi Miyazaki.  (2012-01-14)  Effects of voglibose and nateglinide on glycemic status and coronary atherosclerosis in early-stage diabetic patients..  Circulation journal : official journal of the Japanese Circulation Society,  76  ((3)):  (712-720).  [PMID:22240597]
37. Eberhard Standl,Oliver Schnell.  (2012-04-18)  Alpha-glucosidase inhibitors 2012 - cardiovascular considerations and trial evaluation..  Diabetes & vascular disease research,  ((3)):  (163-169).  [PMID:22508699]
38. Tomoko Kimura,Jinya Suzuki,Mai Ichikawa,Michiko Imagawa,Satsuki Sato,Miki Fujii,Yasuo Zenimaru,Satoru Inaba,Sadao Takahashi,Tadashi Konoshita,Isamu Miyamori.  (2012-04-24)  Differential effects of α-glucosidase inhibitors on postprandial plasma glucose and lipid profile in patients with type 2 diabetes under control with insulin lispro mix 50/50..  Diabetes technology & therapeutics,  14  ((7)):  (545-551).  [PMID:22519736]
39. .  (2012-09-29)  Intestinal alpha-glucosidase inhibitors: abdominal gas cysts..  Prescrire international,  21  ((130)):  (212-213).  [PMID:23016254]
40. Makoto Ayaori,Naotsugu Iwakami,Harumi Uto-Kondo,Hiroki Sato,Makoto Sasaki,Tomohiro Komatsu,Maki Iizuka,Shunichi Takiguchi,Emi Yakushiji,Kazuhiro Nakaya,Makiko Yogo,Masatsune Ogura,Bonpei Takase,Takehiko Murakami,Katsunori Ikewaki.  (2013-03-26)  Dipeptidyl peptidase-4 inhibitors attenuate endothelial function as evaluated by flow-mediated vasodilatation in type 2 diabetic patients..  Journal of the American Heart Association,  ((1)):  (e003277-e003277).  [PMID:23525426]
41. Masayuki Yamaguchi,Takami Saji,Sachiko Mita,Kenneth Kulmatycki,Yan-Ling He,Kenichi Furihata,Kaneo Sekiguchi.  (2013-06-21)  Pharmacokinetic and pharmacodynamic interaction of vildagliptin and voglibose in Japanese patients with Type 2 diabetes..  International journal of clinical pharmacology and therapeutics,  51  ((8)):  (641-651).  [PMID:23782587]
42. Ho-Sook Kim,Minkyung Oh,Eun Ji Kim,Geun Seog Song,Jong-Lyul Ghim,Ji-Hong Shon,Dong-Hyun Kim,Jae-Gook Shin.  (2014-08-28)  Effect of voglibose on the pharmacokinetics of metformin in healthy Korean subjects..  International journal of clinical pharmacology and therapeutics,  52  ((11)):  (1005-1011).  [PMID:25161160]
43. Kaoru Noguchi,Minoru Hirota,Toru Miyoshi,Yoshinori Tani,Yoko Noda,Hiroshi Ito,Seiji Nanba.  (2014-12-03)  Single administration of vildagliptin attenuates postprandial hypertriglyceridemia and endothelial dysfunction in normoglycemic individuals..  Experimental and therapeutic medicine,  ((1)):  (84-88).  [PMID:25452780]
44. Clement Lo,Tadashi Toyama,Ying Wang,Jin Lin,Yoichiro Hirakawa,Min Jun,Alan Cass,Carmel M Hawley,Helen Pilmore,Sunil V Badve,Vlado Perkovic,Sophia Zoungas.  (2018-09-25)  Insulin and glucose-lowering agents for treating people with diabetes and chronic kidney disease..  The Cochrane database of systematic reviews,  ():  (CD011798-CD011798).  [PMID:30246878]
45. Ji-Won Kim,Ye-Jee Lee,Young-Hye You,Min Kyong Moon,Kun-Ho Yoon,Yu-Bae Ahn,Seung-Hyun Ko.  (2018-11-27)  Effect of sodium-glucose cotransporter 2 inhibitor, empagliflozin, and α-glucosidase inhibitor, voglibose, on hepatic steatosis in an animal model of type 2 diabetes..  Journal of cellular biochemistry,    ():  ().  [PMID:30474134]
46. Jin Bong Choi,Je Mo Yoo,Ye-Jee Lee,Jae Woong Kim,Seung-Ju Lee,Hee Youn Kim,Dong Sup Lee,Seung-Hyun Ko,Hyun-Sop Choe.  (2020-04-07)  Effect of the Sodium-Glucose Cotransporter 2 Inhibitor, Dapagliflozin, on Genitourinary Infection in an Animal Model of Type 2 Diabetes..  International neurourology journal,  24  ((1)):  (21-28).  [PMID:32252183]
47. Kentaro Ejiri,Toru Miyoshi,Hajime Kihara,Yoshiki Hata,Toshihiko Nagano,Atsushi Takaishi,Hironobu Toda,Seiji Nanba,Yoichi Nakamura,Satoshi Akagi,Satoru Sakuragi,Taro Minagawa,Yusuke Kawai,Nobuhiro Nishii,Soichiro Fuke,Masaki Yoshikawa,Kazufumi Nakamura,Hiroshi Ito.  (2020-08-18)  Effect of Luseogliflozin on Heart Failure With Preserved Ejection Fraction in Patients With Diabetes Mellitus..  Journal of the American Heart Association,  ((16)):  (e015103-e015103).  [PMID:32805185]
48. Pooja Shah,Vishal Chavda,Snehal Patel,Shraddha Bhadada,Ghulam Md Ashraf.  (2020-10-16)  Promising Anti-stroke Signature of Voglibose: Investigation through In- Silico Molecular Docking and Virtual Screening in In-Vivo Animal Studies..  Current gene therapy,  20  ((3)):  (223-235).  [PMID:33054705]

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