Edoxaban hydrochloride
- Product Name
- Edoxaban hydrochloride
- CAS No.
- 480448-29-1
- Chemical Name
- Edoxaban hydrochloride
- Synonyms
- Edoxaban Hcl;Edoxaban (HCl salt);Edoxaban hydrochloride;Edoxaban Monohydrochloride;N'-(5-chloropyridin-2-yl)-N-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-[(5-methyl-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine-2-carbonyl)amino]cyclohexyl]oxamide:hydrochloride;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]ethanediamide hydrochloride
- CBNumber
- CB42549583
- Molecular Formula
- C24H31Cl2N7O4S
- Formula Weight
- 584.51844
- MOL File
- 480448-29-1.mol
N-Bromosuccinimide Price
- Product number
- API0013888
- Product name
- EDOXABAN HYDROCHLORIDE
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $498.97
- Updated
- 2021/12/16
Edoxaban hydrochloride Chemical Properties,Usage,Production
Description
Edoxaban (Lixiana), a direct inhibitor of Factor Xa (FXa) was approved by the Minister of Health, Labor, and Welfare in Japan in April 2011 for the prevention of venous thromboembolism (VTE) after major orthopedic surgery. Edoxaban inhibits hFXa with a Ki=0.56 nM. Edoxaban is a weak inhibitor of thrombin Ki=6000 nM, has >10,000 fold selectivity over other serine proteases in the coagulation cascade, and demonstrates selectivity over trypsin and chymotrypsin. The synthesis of this class of FXa inhibitors begins with assembly of the diaminocyclohexane scaffold, cis-t-butyl((1R,2S,5S)-2-amino-5-(dimethylcarbamoyl)cyclohexyl)carbamate. The free amine is coupled to the P1 group, 2-((5-chloropyridin-2-yl) amino)-2-oxoacetic acid. The Boc protecting group on the amine of the scaffold is removed and the resulting free amine is coupled to the P4 group, 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid.
Originator
Daiichi Pharmaceutical (Japan)
Uses
Edoxaban (DU-176b) hydrochloride is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban hydrochloride exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban hydrochloride can be used for preventing thromboembolic disease research[1].
brand name
Lixiana
in vivo
Edoxaban hydrochloride (0.5, 2.5 and 12.5 mg/kg; p.o.; once) significantly and dose-dependently reduces the thrombus formation and prolongs PT[1].
| Animal Model: | Male Slc: Wistar rats (210-240 g); Male New Zealand White rabbits(2.5-3.5 kg) (Both are venous stasis thrombosis model)[1]. |
| Dosage: | 0.5, 2.5 and 12.5 mg/kg |
| Administration: | Oral administration; once |
| Result: | Inhibited exogenous FXa activity. Antithrombotic. |
References
[1] Furugohri T, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008 Sep;6(9):1542-9. DOI:10.1111/j.1538-7836.2008.03064.x
Edoxaban hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
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