リナグリプチン
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- CAS番號(hào).
- 668270-12-0
- 化學(xué)名:
- リナグリプチン
- 別名:
- リナグリプチン;リナグリプチン;リナグリプチン (JAN);8-[(3R)-3-アミノピペリジン-1-イル]-7-(2-ブチニル)-3-メチル-1-[(4-メチルキナゾリン-2-イル)メチル]-7H-プリン-2,6-ジオン;8-[(3R)-3-アミノピペリジン-1-イル]-7-(2-ブチン-1-イル)-3-メチル-1-(4-メチルキナゾリン-2-イル)メチル-3,7-ジヒドロ-1H-プリン-2,6-ジオン;8-[(3R)-3-アミノピペリジン-1-イル]-7-(ブタ-2-イン-1-イル)-3-メチル-1-[(4-メチルキナゾリン-2-イル)メチル]-3,7-ジヒドロ-1H-プリン-2,6-ジオン;8-[(3R)-3-アミノピペリジン-1-イル]-7-(2-ブチニル)-3-メチル-1-(4-メチルキナゾリン-2-イルメチル)-3H,7H-プリン-2,6-ジオン;8-[(3R)-3-アミノピペリジン-1-イル]-7-(ブタ-2-イン-1-イル)-3-メチル-1-[(4-メチルキナゾリン-2-イル)メチル]-2,3,6,7-テトラヒドロ-1H-プリン-2,6-ジオン;トラゼンタ;8-[(3R)-3-アミノピペリジン-1-イル]-7-(2-ブチニル)-3-メチル-1-[(4-メチルキナゾリン-2-イル)メチル]-3,7-ジヒドロ-1H-プリン-2,6-ジオン
- 英語(yǔ)名:
- Linagliptin
- 英語(yǔ)別名:
- Linagliptin API;Linaglitpin;Linagliptin (BI-1356);8-[(3R)-3-Amino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione;inag;iptin;inagL;Ondero;CS-494;Bi 1356
- CBNumber:
- CB71518518
- 化學(xué)式:
- C25H28N8O2
- 分子量:
- 472.54
- MOL File:
- 668270-12-0.mol
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リナグリプチン 物理性質(zhì)
- 融點(diǎn) :
- 202 ºC
- 沸點(diǎn) :
- 661.2±65.0 °C(Predicted)
- 比重(密度) :
- 1.39
- 貯蔵溫度 :
- Refrigerator
- 溶解性:
- クロロホルム（少量）、DMSO（少量）、メタノール（少量）
- 酸解離定數(shù)(Pka):
- 10.01±0.20(Predicted)
- 外見(jiàn) :
- 個(gè)體
- 色:
- 白からオレンジ
- InChIKey:
- LTXREWYXXSTFRX-QGZVFWFLSA-N
- SMILES:
- N1(CC#CC)C2=C(N(C)C(=O)N(CC3=NC(C)=C4C(=N3)C=CC=C4)C2=O)N=C1N1CCC[C@@H](N)C1
リナグリプチン 価格
| メーカー |
製品番號(hào) |
製品説明 |
CAS番號(hào) |
包裝 |
価格 |
更新時(shí)間 |
購(gòu)入 |
リナグリプチン 化學(xué)特性,用途語(yǔ),生産方法
効能
糖尿病治療薬, DPP-4阻害薬
商品名
トラゼンタ (日本ベーリンガーインゲルハイム)
説明
Linagliptin (trade names Tradjenta and Trajetna) is an inhibitor of
dipeptidyl peptidase-4 (DPP-4) that was approved by the U.S. FDA in May
2011 for the treatment of Type 2 diabetes along with diet and exercise.
Linagliptin (BI-1356) has been
described as a potent highly selective, slow-off rate and long acting inhibitor of DPP-4. Linagliptin arose from optimization efforts of xanthine-based
DPP-4 inhibitors with the initial lead identified from an HTS campaign.
After optimizing the activity of the initial micromolar lead, two issues that needed to be addressed were activity for hERG and muscarinic receptor M1.
Introduction of a butynyl group at the N7 position of the xanthine ring gave
much reduced M1 affinity with no measureable hERG activity. Linagliptin
inhibits DPP-4 with an IC
50=1 nM and is highly selective (>10,000-fold)
against DPP-8 and DPP-9. Linagliptin shows no interactions with CYPs up
to 50 mM. The described synthesis of linagliptin starts with 8-bromoxanthine,
which is alkylated at the N-7 position to introduce the butyne group,
followed by alkylation of the N-1 group to introduce the methyl-quinazoline
group. Displacement of the bromide with (R)-Boc-3-amino-piperidine
followed by deprotection gives linagliptin. When administered to db/db
mice orally, linagliptin dose dependently reduced glucose excursion from
0.1 mg/kg (15% inhibition) to 1 mg/kg (66% inhibition).
使用
Labeled Linagliptin, intended for use as an internal standard for the quantification of Linagliptin by GC- or LC-mass spectrometry.
定義
ChEBI: A xanthine that is 7H-xanthine bearing (4-methylquinazolin-2-yl)methyl, methyl, but-2-yn-1-yl and 3-aminopiperidin-1-yl substituents at positions 1, 3, 7 and 8 respectively (the R-enantiomer). Used for treatment of type
I diabetes.
リナグリプチン 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品
リナグリプチン 生産企業(yè)
Global( 657)Suppliers
668270-12-0(リナグリプチン)キーワード:
- 668270-12-0
- linagliptin
- (R)-8-(3-Amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione
- 1H-Purine-2,6-dione, 8-((3R)-3-amino-1-piperidinyl)-7-(2-butynyl)-3,7-dihydro-3-methyl-1-((4-methyl-2-quinazolinyl)methyl)-
- Bi 1356
- Ondero
- 8-[(3R)-3-AMino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-Methyl-1-[(4-Methyl-2-quinazolinyl)Methyl]-1H-purine-2,6-dione
- 8-[(3R)-3-AMino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-Methyl-1-[(4-Methyl-2-quinazolinyl)Methyl]-1H-purine-2,6-d
- 8-[(3R)-3-aMinopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-Methyl-1-[(4-Methylquinazolin-2-yl)Methyl]-2,3,6,7-tetrahydro-1H-purine-2,6-dione
- Tradjenta
- Linagliptin-D4
- Linaglitine
- (R)-8-(3-aMinopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-Methyl-1-((4-Methylquinazolin-2-yl)Methyl)-1H-purine-2,6(3H,7H)-dione
- 1H-Purine-2,6-dione,8-[(3R)-3-aMino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-Methyl-1-[(4-Methyl-2-quinazolinyl)Methyl]-
- (R)-8-(3-aminopiperidin-1-yl)-7-(but-2-ynyl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione
- Linagliptin
8-[(3R)-3-Amino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione
- Linagliptin, >=98%
- linagliptin / 1H-Purine-2,6-dione, 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-
- Linagliptin (668270-12-0)
- 8-[(3R)-3-AMino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-Met
- Lillidine
- CS-1974
- CS-494
- BI1356; BI 1356
- Lilalitine
- inag
- iptin
- inagL
- Linagliptin ISO 9001：2015 REACH
- Linagliptin Impurity 81
- Linagliptin Impurity 79
- リナグリプチン
- リナグリプチン
- リナグリプチン (JAN)
- 8-[(3R)-3-アミノピペリジン-1-イル]-7-(2-ブチニル)-3-メチル-1-[(4-メチルキナゾリン-2-イル)メチル]-7H-プリン-2,6-ジオン
- 8-[(3R)-3-アミノピペリジン-1-イル]-7-(2-ブチン-1-イル)-3-メチル-1-(4-メチルキナゾリン-2-イル)メチル-3,7-ジヒドロ-1H-プリン-2,6-ジオン
- 8-[(3R)-3-アミノピペリジン-1-イル]-7-(ブタ-2-イン-1-イル)-3-メチル-1-[(4-メチルキナゾリン-2-イル)メチル]-3,7-ジヒドロ-1H-プリン-2,6-ジオン
- 8-[(3R)-3-アミノピペリジン-1-イル]-7-(2-ブチニル)-3-メチル-1-(4-メチルキナゾリン-2-イルメチル)-3H,7H-プリン-2,6-ジオン
- 8-[(3R)-3-アミノピペリジン-1-イル]-7-(ブタ-2-イン-1-イル)-3-メチル-1-[(4-メチルキナゾリン-2-イル)メチル]-2,3,6,7-テトラヒドロ-1H-プリン-2,6-ジオン
- トラゼンタ
- 8-[(3R)-3-アミノピペリジン-1-イル]-7-(2-ブチニル)-3-メチル-1-[(4-メチルキナゾリン-2-イル)メチル]-3,7-ジヒドロ-1H-プリン-2,6-ジオン