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カナグリフロジン

カナグリフロジン 化学構造式
842133-18-0
CAS番号.
842133-18-0
化学名:
カナグリフロジン
别名:
カナグリフロジン
英語化学名:
Canagliflozin
英語别名:
CS-183;TA 7284;Invokana;Cagliflozin;Canaglifozin;Canagliflozi;JNJ 28431754;Canaglifozion;Canagliflozin;JNJ 24831754ZAE
CBNumber:
CB02510088
化学式:
C24H25FO5S
分子量:
444.5157032
MOL File:
842133-18-0.mol

カナグリフロジン 物理性質

沸点 :
642.9±55.0 °C(Predicted)
比重(密度) :
1.364
酸解離定数(Pka):
13.34±0.70(Predicted)
CAS データベース:
842133-18-0

安全性情報

カナグリフロジン 価格

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入

カナグリフロジン 化学特性,用途語,生産方法

説明

In March 2013, the US FDA approved canagliflozin (JNJ-28431754; TA-7284) for the treatment of type 2 diabetes in adults. Canagliflozin is the first US-approved sodium-glucose co-transporter (SGLT) inhibitor for the treatment of type 2 diabetes. Inhibition of renal SGLT suppresses glucose reabsorption, which permits glucose excretion into urine and reduction of hyperglycemia. Canagliflozin was discovered through structural modifications of phlorizin, a known inhibitor of renal glucose reabsorption. Early modifications of OH groups on the glucose moiety were insufficient to adequately impair hydrolysis by intestinal β-glucosidase. Introduction of the C-glucoside moiety, as in the clinical candidate dapagliflozin, afforded sufficient resistance to hydrolysis. Finally, incorporation of the thiophene moiety in canagliflozin provided improved potency for hSGLT2 (exclusive to kidney), IC50=2.2 nM, while offering significant selectivity over hSGLT1 (in kidney and heart), IC50=910 nM. Hyperglycemic, high-fat (HF) diet fedmice (KKstrain) that received a single 3 mg/kg oral dose of canagliflozin had a 48% reduction in blood glucose levels after 6 h versus vehicle-treatedmice. Noteworthy in themultistep synthesis of canagliflozin is the stereoselective formation of the β-C-glucoside which is accomplished by coupling of the aryllithiumaglycone with 2,3,4,6-tetra-O-trimethylsilyl-β-Dgluconolactone followed by desilylation and stereoselective reduction with triethylsilane and boron trifluoride etherate.

化学的特性

Pale Yellow Solid

Originator

Mitsubishi Tanabe Pharma (Japan)

使用

Canagliflozin is a sodium/glucose cotransporter 2 (SGLT2) inhibitor. Canagliflozin has been shown to dose dependently reduce calculated renal threshold for glucose excretion and increase urinary glucose excretion. Canagliflozin is a candidate for the treatment of type 2 diabetes and obesity.

定義

ChEBI: A C-glycosyl compound that is used (in its hemihydrate form) for treatment of type II diabetes via inhibition of sodium-glucose transport protein subtype 2.

brand name

Invokana

カナグリフロジン 上流と下流の製品情報

原材料

準備製品


カナグリフロジン 生産企業

Global( 269)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Echemi Group
18905328650 86-18905328650
pharma@echemi.com CHINA 194 58
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21838 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22625 55
Hangzhou FandaChem Co.,Ltd.
0086 158 5814 5714 (Mobile
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Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24754 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 341 58
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 296 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30043 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 968 58

842133-18-0(カナグリフロジン)キーワード:


  • 842133-18-0
  • CS-183
  • TA 7284
  • Canaglifozion
  • Cango coluMn net
  • D-Glucitol, 1,5-anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]Methyl]-4-Methylphenyl]-, (1S)-
  • Cagliflozin
  • Invokana
  • Canagliflozin(TA-7284)
  • (2S,3R,4R,5S,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol
  • Canaglifozin
  • Canagliflozin WS
  • Canagliflozi
  • (1S)-1,5-Anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-D-glucitol
  • Canagliflozin, >=98%
  • Canagliflozin-D6
  • D-Glucitol, 1,5-anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]Methyl]-4-Methylphenyl
  • (1S)-1,5-anhydro-1-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4 -methylphenyl]-D-glucitol
  • JNJ 24831754ZAE
  • JNJ 28431754
  • JNJ 28431754AAA
  • Canagliflozin
  • カナグリフロジン
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