Linagliptin
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- CAS-Nr.
- 668270-12-0
- Englisch Name:
- Linagliptin
- Synonyma:
- Linagliptin-D4;Linagliptin API;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;Linaglitpin;Linagliptin (BI-1356);inag;iptin;inagL;Ondero;CS-494
- CBNumber:
- CB71518518
- Summenformel:
- C25H28N8O2
- Molgewicht:
- 472.54
- MOL-Datei:
- 668270-12-0.mol
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Linagliptin Eigenschaften
- Schmelzpunkt:
- 202 ºC
- Siedepunkt:
- 661.2±65.0 °C(Predicted)
- Dichte
- 1.39
- storage temp.
- Refrigerator
- L?slichkeit
- Chloroform (Sparingly), DMSO (Slightly), Methanol (Slightly)
- pka
- 10.01±0.20(Predicted)
- Aggregatzustand
- Solid
- Farbe
- White to Orange
- 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
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung
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| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
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P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
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P264, P280, P305+P351+P338,P337+P313P |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizit?t (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
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| Sicherheit |
| P264 |
Nach Gebrauch gründlich waschen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
| P302+P352 |
BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
| P321 |
Besondere Behandlung |
| P332+P313 |
Bei Hautreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
| P362 |
Kontaminierte Kleidung ausziehen und vor erneutem Tragen waschen. |
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Linagliptin Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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).
Verwenden
Labeled Linagliptin, intended for use as an internal standard for the quantification of Linagliptin by GC- or LC-mass spectrometry.
Definition
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.
Linagliptin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Linagliptin Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 718)Lieferanten
668270-12-0()Verwandte Suche:
- 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
- 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
- (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,8H)-dione
- LinagliptinQ: What is
Linagliptin Q: What is the CAS Number of
Linagliptin Q: What is the storage condition of
Linagliptin Q: What are the applications of
Linagliptin
- Azelastina
- Azelastinum
- Linagliptin (BI-1356)
- Linagliptin API
- Linaglitpin
- Benzene,1,2-dichloro-9-methoxy-
- 2-Pyrrolidinone,10-(hydroxymethyl)-
- LIGLIPTIN
- Liggliptin
- Linagliptin
(R)-8-(3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4- methylquinazolin-2-yl)methyl)-3,7-dihydro-1H-purine-2,6-dione
- Liraglutine
- Ligagliptin
- 668270-12-0
- Linagliptin, 10 mM in DMSO
- LINAGLIPTIN, NON-STERILE BULK DRUG SUBSTANCE
- Linagliptin - Mix of Form A and B
- Linagliptin - Bio-X ?
- Linagliptin (GSK2118436)
- Linagliptin (under development)
- (r)-8-(3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-3,7-dihydro-1h-purine-2,6-dione
- (R)-8-[3-Aminopiperidin-1-yl]-7-(2-butynyl)-3-methyl-1-(4-methylquinazolin-2-ylmethyl)xanthine
- 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-D4
- Lilalitidine
- 668270-12-0
- 6668270-12-0
- 68270-12-0
