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edoxaban

Product Name
edoxaban
CAS No.
480449-70-5
Chemical Name
edoxaban
Synonyms
Edoxaban base;EthanediaMide, N1-(5-chloro-2-pyridinyl)-N2-[(1S,2R,4S)-4-[(diMethylaMino)carbonyl]-2-[[(4,5,6,7-tetrahydro-5-Methylthiazolo[5,4-c]pyridin-2-yl)carbonyl]aMino]cyclohexyl]-;DU-176;edoxaban;Edoxaban(DU-176);edoxaban USP/EP/BP;edoxaban480449-70-5;Edoxaban/Ethanediamide;Edoxaban (See C3D-1344);Tropicamide Impurity 34
CBNumber
CB21518508
Molecular Formula
C24H30ClN7O4S
Formula Weight
548.06
MOL File
480449-70-5.mol
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edoxaban Property

Melting point:
>213°C (dec.)
Density 
1.43
storage temp. 
Hygroscopic, Refrigerator, under inert atmosphere
solubility 
Chloroform (Slightly), DMSO (Slightly, Heated), Methanol (Slightly, Heated)
pka
9.46±0.70(Predicted)
form 
Solid
color 
White to Off-White
InChI
InChI=1S/C24H30ClN7O4S/c1-31(2)24(36)13-4-6-15(27-20(33)21(34)30-19-7-5-14(25)11-26-19)17(10-13)28-22(35)23-29-16-8-9-32(3)12-18(16)37-23/h5,7,11,13,15,17H,4,6,8-10,12H2,1-3H3,(H,27,33)(H,28,35)(H,26,30,34)/t13-,15-,17+/m0/s1
InChIKey
HGVDHZBSSITLCT-JLJPHGGASA-N
SMILES
C(NC1=NC=C(Cl)C=C1)(=O)C(N[C@H]1CC[C@H](C(N(C)C)=O)C[C@H]1NC(C1=NC2CCN(C)CC=2S1)=O)=O
LogP
-1.455
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Safety

Hazardous Substances Data
480449-70-5(Hazardous Substances Data)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H373May cause damage to organs through prolonged or repeated exposure

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P314Get medical advice/attention if you feel unwell.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

TRC
Product number
E555520
Product name
Edoxaban
Packaging
5mg
Price
$95
Updated
2021/12/16
AK Scientific
Product number
X1006
Product name
Edoxaban
Packaging
25mg
Price
$126
Updated
2021/12/16
AK Scientific
Product number
J98273
Product name
Edoxaban
Packaging
50mg
Price
$150
Updated
2021/12/16
ChemScene
Product number
CS-1331
Product name
Edoxaban
Purity
99.03%
Packaging
10mg
Price
$160
Updated
2021/12/16
Matrix Scientific
Product number
098152
Product name
Edoxaban
Purity
95+%
Packaging
250mg
Price
$264
Updated
2021/12/16
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edoxaban Chemical Properties,Usage,Production

Uses

oral factor Xa inhibitor

Uses

Edoxaban is an anticoagulant drug which acts as a direct factor Xa inhibitor.

Definition

ChEBI: A monocarboxylic acid amide that is used (as its tosylate monohydrate) for the treatment of deep vein thrombosis and pulmonary embolism.

Indications

Edoxaban is a direct oral anticoagulant (DOAC). It exerts its effects by inhibiting factor Xa (FXa). Edoxaban was FDA approved in early 2015 to treat deep venous thrombosis, pulmonary embolism and decrease the risk of hypercoagulability related illness; stroke, and systemic embolism (SE) in subjects with nonvalvular atrial fibrillation (NVAF).When compared to the popularly used anticoagulant warfarin, edoxaban entails more limited monitoring and possesses a reduced risk for significant bleeding and fewer interactions with other agents.Edoxaban is the most current direct oral anticoagulant (DOAC) and does not associate with the CYP-450 system.
Various clinical trials and studies (ENGAGE AF-TIMI and Hokusai-VTE) expressed edoxaban's effectiveness compared to the conventional vitamin K antagonist warfarin. It was demonstrated to be non-inferior in preventing blood clots when compared to warfarin. Edoxaban is the second FDA-approved anticoagulant agent with once-daily administration.Contrary to the other direct oral anticoagulants, apixaban and rivaroxaban, edoxaban has not yet received approval for secondary and postoperative prophylaxis for venous thromboembolism (VTE).
FDA-Approved Indications:
Deep venous thrombosis
Pulmonary embolism
Nonvalvular atrial fibrillation (NVAF)
https://www.ncbi.nlm.nih.gov/

Pharmacology

Similar to rivaroxaban and apixaban,edoxaban is an orally active, small-molecule (548 Da), reversible factor Xa inhibitor.As with the other direct oral factor Xa inhibitors,edoxaban exhibits a 10,000-fold greater selectivity for factor Xa compared with other serine proteins such as factor VlIa, t-PA, plasmin,or trypsin.Administered as edoxaban tosylate,the compound competitively inhibits free factor Xa directly without the need for antithrombin and factor Xa incorporated in the prothrombinase complex. The concentration-dependent inhibition of factor Xa leads to reduced thrombin generation and thrombin-induced platelet aggregation. Edoxaban inhibited factor Xa with Ki values of 0.561 nM for free factor Xa and 2.98 nM for prothrombinase.128 Edoxaban exhibits linear pharmacokinetics and produces concentration-dependent increases in the PT,INR, and aPTT.However,changes in these laboratory assays with edoxaban tend to be unpredictable and highly variable, reducing their use as a monitoring tool in clinical practice.
Pharmacokinetics and Pharmacodynamics of Edoxaban, a Non-Vitamin K Antagonist Oral Anticoagulant that Inhibits Clotting Factor Xa
Laboratory measurement of the anticoagulant activity of edoxaban: a systematic review
Pharmacokinetics, biotransformation, and mass balance of edoxaban, a selective, direct factor Xa inhibitor, in humans

target

factor Xa

Drug interactions

The majority of edoxaban pharmacokinetic drug interactions result from inhibition or induction of the P-gp efflux transporter,which is responsible for intestinal transport.Edoxaban taken with quinidine demonstrates an increase in edoxaban Cmax of 85% and AUS of 77%.Coadministration with dronedarone resulted in a Cmax and AUC increase of 46% and 85%,respectively.This drug interaction also increased the 24-h edoxaban concentration by 158%.Additionally, verapamil increased the edoxaban Cmax by 53%, the AUC by 53%, and the 24-h edoxaban concentration by 29%.146 As per the phase 3 clinical trial, patients receiving quinidine, dronedarone,or verapamil should receive the reduced dose of 30 mg daily instead of 60 mg daily.It should be noted that patients receiving azole antifungal agents, such as ketoconazole, or protease inhibitors were excluded from the phase 3 trial because of concerns about increased edoxaban exposure.Conversely, the use of rifampin, a P-gp inducer, resulted in a significant 34% reduction in the edoxaban AUC.Therefore, the combination of rifampin and edoxaban should be avoided.

edoxaban Preparation Products And Raw materials

Raw materials

Preparation Products

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edoxaban Suppliers

Jiangsu Vcare PharmaTech Co., Ltd.
Tel
025-58741518; 18013018875
Fax
+86-25-58744115
Email
sales@vcarepharmatech.com
Country
China
ProdList
310
Advantage
61
iangsu U-Liy Biotech Pharmaceuticals Inc
Tel
18021412923
Email
1515809609@qq.com
Country
China
ProdList
141
Advantage
58
Jiangsu Simcere Pharmaceutical CO.,Ltd
Tel
025-85566666-8770 15195996671
Email
API@simcere.com
Country
China
ProdList
19
Advantage
58
Jiangxi ravel Biotechnology Co.,Ltd
Tel
400-880-2824 15608648206
Email
1987516016@qq.com
Country
China
ProdList
2772
Advantage
58
Jiangxi Zhiyan Biopharmaceutical Technology Co., Ltd
Tel
13732973797
Email
liu@zybiopharma.com
Country
China
ProdList
270
Advantage
58
Jinan zhongdaoanran chemical Co;Ltd
Tel
18678233466 18678233466
Email
122574856@qq.com
Country
China
ProdList
65
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chemvon Biotechnology Co., Ltd
Tel
021-50790412
Fax
+86-21-50790419
Email
info@chemvon.com
Country
China
ProdList
371
Advantage
57
Suzhou Zehou Biotechnology Co. , Ltd.
Tel
0512-68716880 18075373931
Fax
18075373931
Email
sales@growingchem.com
Country
China
ProdList
191
Advantage
64
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
Advantage
58
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View Lastest Price from edoxaban manufacturers

Jinan Million Pharmaceutical Co., Ltd
Product
edoxaban 480449-70-5
Price
US $1.00/kg
Min. Order
0.10000000kg
Purity
99%
Supply Ability
200KG
Release date
2024-08-21
Sinoway Industrial co., ltd.
Product
Edoxaban 480449-70-5
Price
US $235.00-85.00/Kg/Bag
Min. Order
1Kg/Bag
Purity
99% up, High Density
Supply Ability
20 tons
Release date
2023-12-06
WUHAN FORTUNA CHEMICAL CO., LTD
Product
Edoxaban 480449-70-5
Price
US $0.00/KG
Min. Order
10g
Purity
99%min
Supply Ability
10kg
Release date
2021-09-13

480449-70-5, edoxabanRelated Search:


  • Edoxaban base
  • EthanediaMide, N1-(5-chlo...
  • EthanediaMide, N1-(5-chloro-2-pyridinyl)-N2-[(1S,2R,4S)-4-[(diMethylaMino)carbonyl]-2-[[(4,5,6,7-tetrahydro-5-Methylthiazolo[5,4-c]pyridin-2-yl)carbonyl]aMino]cyclohexyl]-
  • edoxaban
  • N-(5-Chloro-2-pyridinyl)-N'-[(1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-[[(4,5,6,7-tetrahydro-5-methylthiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]ethanediamide
  • DU-176
  • Edoxaban(DU-176)
  • Edoxaban N-(5-Chloro-2-pyridinyl)-N'-[(1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-[[(4,5,6,7-tetrahydro-5-methylthiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]ethanediamide
  • 5- chloro -2- pyridine -N, N-dimethyl formamidine
  • Edoxaban Tosylate Hydrate 2
  • edoxaban480449-70-5
  • N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-(dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)cyclohexyl)oxalamide
  • edoxaban USP/EP/BP
  • N-(5-Chloro-2-pyridyl)-N'-(1S,2R,4S)-4-(dimethylcarbamoyl)-2-(5-methyl-6,7-dihydro-4H-thiazolo5,4-cpyridine-2-carbonyl)aminocyclohexyloxamide
  • N'-(5-chloropyridin-2-yl)-N-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-{5-methyl-4H,5H,6H,7H-[1,3]thiazolo[5,4-c]pyridine-2-amido}cyclohexyl]ethanediamide
  • Edoxaban (See C3D-1344)
  • 1H-Imidazole,1-[2,6-bis(5-methylethyl)phenyl]-
  • Edoxaban/Ethanediamide
  • Tropicamide Impurity 34
  • 480449-70-5
  • C24H30ClN7O4S