カナグリフロジン
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- 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;1-[4-メチル-3-[[5-(4-フルオロフェニル)-2-チエニル]メチル]フェニル]-1-デオキシ-β-D-グルコピラノース;1-[3-[[5-(4-フルオロフェニル)-2-チエニル]メチル]-4-メチルフェニル]-1-デオキシ-β-D-グルコピラノース;2-(4-フルオロフェニル)-5-[2-メチル-5-(β-D-グルコピラノシル)ベンジル]チオフェン;(1S)-1,5-アンヒドロ-1-[3-[[5-(4-フルオロフェニル)-2-チエニル]メチル]-4-メチルフェニル]-D-グルシトール;(2S,3R,4R,5S,6R)-2-(3-{[5-(4-フルオロフェニル)チオフェン-2-イル]メチル}-4-メチルフェニル)-6-(ヒドロキシメチル)オキサン-3,4,5-トリオール
- 英語名:
- Canagliflozin
- 英語别名:
- Canaglifozin;Invokana;Cagliflozin;JNJ 28431754;Canaglifozion;(1S)-1,5-anhydro-1-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4 -methylphenyl]-D-glucitol;(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;CS-183;TA 7284;Calaglizin
- CBNumber:
- CB02510088
- 化学式:
- C24H25FO5S
- 分子量:
- 444.52
- MOL File:
- 842133-18-0.mol
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カナグリフロジン 物理性質
- 融点 :
- 68 - 72°C
- 沸点 :
- 642.9±55.0 °C(Predicted)
- 比重(密度) :
- 1.364
- 貯蔵温度 :
- -20°C
- 溶解性:
- DMSOに可溶 (40 mg/ml)
- 外見 :
- 個体
- 酸解離定数(Pka):
- 13.34±0.70(Predicted)
- 色:
- 白い
- 安定性：:
- -20°C の DMSO 溶液で最大 1 か月間保存できます。
- InChIKey:
- XTNGUQKDFGDXSJ-XDLHWMRXNA-N
- SMILES:
- O[C@@H]1[C@H]([C@H](O)[C@@H](CO)O[C@H]1C1C=CC(C)=C(CC2=CC=C(C3C=CC(F)=CC=3)S2)C=1)O |&1:1,2,3,5,9,r|
- CAS データベース:
- 842133-18-0
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), IC
50=2.2 nM, while offering significant selectivity over hSGLT1 (in kidney and heart), IC
50=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
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.
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( 476)Suppliers
842133-18-0(カナグリフロジン)キーワード:
- 842133-18-0
- Canaglifozion
- D-Glucitol, 1,5-anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]Methyl]-4-Methylphenyl]-, (1S)-
- Cango coluMn net
- TA 7284
- Cagliflozin
- CS-183
- 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, >=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
- Canagliflozin WS
- Canagliflozi
- (1S)-1,5-Anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-D-glucitol
- JNJ 24831754ZAE
- JNJ 28431754
- JNJ 28431754AAA
- Canagliflozin
- Canagliflozin USP/EP/BP
- (2S,3R,4R,5S,6R)-2-[3-[[5-(4-fluorophenyl)thiophen-2-yl]methyl]-4-methylphenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
- Canagliflozin (JNJ 28431754)
- CanagliflozinQ: What is
Canagliflozin Q: What is the CAS Number of
Canagliflozin Q: What is the storage condition of
Canagliflozin Q: What are the applications of
Canagliflozin
- Kangglijing
- Calaglizin
- JNJ 24831754
- JNJ24831754
- JNJ-24831754
- カナグリフロジン
- 1-[4-メチル-3-[[5-(4-フルオロフェニル)-2-チエニル]メチル]フェニル]-1-デオキシ-β-D-グルコピラノース
- 1-[3-[[5-(4-フルオロフェニル)-2-チエニル]メチル]-4-メチルフェニル]-1-デオキシ-β-D-グルコピラノース
- 2-(4-フルオロフェニル)-5-[2-メチル-5-(β-D-グルコピラノシル)ベンジル]チオフェン
- (1S)-1,5-アンヒドロ-1-[3-[[5-(4-フルオロフェニル)-2-チエニル]メチル]-4-メチルフェニル]-D-グルシトール
- (2S,3R,4R,5S,6R)-2-(3-{[5-(4-フルオロフェニル)チオフェン-2-イル]メチル}-4-メチルフェニル)-6-(ヒドロキシメチル)オキサン-3,4,5-トリオール