Dapagliflozin Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

The Australian Therapeutic Goods Administration (TGA) and the European Commission approved dapagliflozin in October and November 2012, respectively, as an adjunct to diet and exercise for the treatment of type 2 diabetes. Dapagliflozin is a potentially attractive therapy due to its glucosesensitive and insulin-independent mechanism of action. It is a first-in-class selective SGLT2 inhibitor (IC₅₀=1.1 nM; selectivity vs. SGLT1 >1000) that lowers the renal threshold for reabsorption of glucose, allowing excess glucose to be eliminated via the kidneys. In normal rats, administration of dapagliflozin promotes dose-dependent excretion of up to 1900 mg of glucose over a 24 h period, with amaximal effect at 3 mg/kg. In a ratmodel of diabetes, pretreatment with the pancreatic toxin streptozotocin results in hyperglycemia that is reduced 55% by administration of a single 0.1 mg/kg dose of dapagliflozin compared with vehicle. Aryl O-glucoside SGLT2 inhibitors were early entrants into the clinic, but the aryl C-glucoside linkage found in dapagliflozin confers resistance to glucosidase-mediated metabolism leading to improved clinical utility relative to aryl O-glucosides. The modified carbohydrate–aglycone linkage required concomitant adjustment from an ortho- to a meta-substituted arylglucoside to achieve potent SGLT2 inhibition. Dapagliflozin was synthesized in several steps via reaction of an aryllithium with per-silylated gluconolactone to form the key C-glucoside linkage. An alpha-selective reduction of the resultant anomeric glycoside gave the desired beta-Carylglucoside. The main circulating (inactive) metabolite is the result of 3-O-glucuronidation of the glucosylmoiety. Of the minority metabolites, the main oxidative species result from O-dealkylation of the ethoxy-group and hydroxylation of the biarylmethane moiety.

Chemische Eigenschaften

White Solid

Verwenden

A sodium-glucose transporter 2 inhibitor.

Definition

ChEBI: A C-glycosyl comprising beta-D-glucose in which the anomeric hydroxy group is replaced by a 4-chloro-3-(4-ethoxybenzyl)phenyl group. Used (in the formo f its propanediol monohydrate) to improve glycemic ontrol, along with diet and exercise, in adults with type 2 diabetes.

Dapagliflozin Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Dapagliflozin Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Senova Technology Co. Ltd.	+86-0755-86703119 +8618503098836	info@senovatech.com	China	351	58
Hubei Ipure Biology Co., Ltd	+8613367258412	ada@ipurechemical.com	China	10319	58
Baoji Guokang Bio-Technology Co., Ltd.	0917-3909592 13892490616	gksales1@gk-bio.com	China	9312	58
Changzhou Rokechem Technology Co., Ltd.	18758118018	sales001@rokechem.com	China	255	58
Protheragen-ING	+16313385890	info@protheragen-ing.com	United States	3868	58
Sinoway Industrial co., ltd.	0592-5800732; +8613806035118	xie@china-sinoway.com	China	988	58
shandong perfect biotechnology co.ltd	+86-53169958659 +86-13153181156	sales@sdperfect.com	China	294	58
Hangzhou ICH Biofarm Co., Ltd	+86-0571-28186870; +undefined8613073685410	sales@ichemie.com	China	1001	58
Hebei Xinsheng New Material Technology Co., LTD.	+86-16632316109	xinshengkeji@xsmaterial.com	China	1085	58
Anhui Ruihan Technology Co., Ltd	+8617756083858	daisy@anhuiruihan.com	China	973	58

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• Dapagliflozin(BMS-512148)
• 1-[4-Chloro-3-(4-ethoxybenzyl)phenyl]-1-deoxy-beta-D-glucopyranose (1S)-1,5-Anhydro-1-C-[4-chloro-3-(4-ethoxybenzyl)phenyl]-D-glucitol (2S,3R,4R,5S,6R)-2-[4-Chloro-3-(4-ethoxybenzyl)phenyl]-6-(hydroxyMethyl)tetrahydro-2H-pyran-3,4,5-triol
• (2S,3R,4R,5S,6R)-2-(3-(4-ethoxybenzyl)-4-chlorophenyl)-6-hydroxyMethyltetrahydro-2H-pyran-3,4,5-triol
• 1-[4-Chloro-3-(4-ethoxybenzyl)phenyl]-1-deoxy-beta-D-glucopyranose
• BMS5121458
• Dag coluMn net
• Dapagliflozin Isomer Impurity
• Dapagliflozin, >=98%
• DAPAGLIFLOZIN
• BMS-512148-05
• Bms 512148
• apagliflozin
• Dapagliflozin USP/EP/BP
• Dagagflozin
• Dagliejing
• Dapagliflozin S1548 Selleck
• Daglican
• CS-179
• Dagliel
• Dapagli ozin
• Dapagliflozen amorphous
• High Quality Dapagliflozin CAS No. 461432-26-8 with Safe Shipping
• (2S,3R,4R,5S,6R)-2-[4-Chloro-3-(4-ethoxybenzyl)phenyl]-6-(hy...
• DapagliflozinQ: What is Dapagliflozin Q: What is the CAS Number of Dapagliflozin Q: What is the storage condition of Dapagliflozin Q: What are the applications of Dapagliflozin
• Dapagliflozin Propanediol Monohydrate
• (1S)-1,5-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-D-glucitol
• Dapagliflozin propanediol
• Farxiga
• DAPAGLIFLOZIN BASE
• Dapagliflozi
• D-Glucitol, 1,5-anhydro-1-C-(4-chloro-3-((4-ethoxyphenyl)methyl)phenyl)-, (1S)-
• (2S,4R,5R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(hydroxyMethyl)tetrahydro-2H-pyran-3,4,5-triol
• 2-(3-(4-Ethoxybenzyl)-4-chlorophenyl)-6-hydroxymethyltetrahydro-2H-pyran-3,4,5-triol
• Glenn net
• DAPAGLIFLOZIN（base，Amorphous）
• (1S)-1,5- dehydration -1-C-[4- chloro -3-[(4- ethoxyphenyl) methyl] phenyl ]-D- glucitol
• BMS512148,Sodium-dependent glucose cotransporters,SGLT,BMS 512148,inhibit,Dapagliflozin,Inhibitor
• (2S,3R,4R,5S,6R)-2-{4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl}-6-(hydroxymethyl)oxane-3,4,5-triol
• Dapagliflozin CRS
• Dagliflozin
• 2-Chloro-5-（ β- D-glucopyrano-1-yl) -4 '- ethoxydiphenylmethane
• Dapagliflozin (Propanediol Monohydrate & Amorphous)
• Dapgliflozin
• Dapagliflozin Reference Standard
• Dagliazine
• 461432-26-8
• 461432-26-8;960404-48-2
• 61432-26-8
• 46132-26-8
• 461436-26-8
• C21H25ClO6
• Inhibitors
• Other APIs
• APIs
• Aromatics
• Heterocycles
• Intermediates & Fine Chemicals
• Pharmaceuticals