- PPACK Dihydrochloride
- 5-R-Rivaroxaban
- Bivalirudin Trifluoroacetate
- Dabigatran etexilate mesylate
- Dabigatran ethyl ester
| BIBR-1048Thrombin inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.89%
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Chemical structure
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| Cas No. | 211915-06-9 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | ethyl 3-[[2-[[4-[(Z)-N"-hexoxycarbonylcarbamimidoyl]anilino]methyl]-1-methylbenzimidazole-5-carbonyl]-pyridin-2-ylamino]propanoate | ||
| Canonical SMILES | CCCCCCOC(=O)N=C(C1=CC=C(C=C1)NCC2=NC3=C(N2C)C=CC(=C3)C(=O)N(CCC(=O)OCC)C4=CC=CC=N4)N | ||
| Formula | C34H41N7O5 | M.Wt | 627.73 |
| Solubility | ≥30 mg/mL in DMSO, <3.1 mg/ml="" in="" h2o,="" ≥22.13="" mg/ml="" in="" etoh=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Dabigatran etexilate is a potent, selective and competitive inhibitor of thrombin. It is an oral prodrug of dabigatran. Ki=4.5 nM for human thrombin and IC50=10 nM for thrombin-induced platelet aggregation. [1] [2]
Thrombin is protein that proteolytically cleaved from coagulation factor II as the initial step in the coagulation cascade. It transforms fibrinogen into fibrin and activates other factors in function in blood homeostasis, wound healing and inflammation.
In vitro, dabigatran showed anticoagulant effects in a concentration-dependent manner. It doubled the activated partrial thromboplastin time, prothrombin time and ecarin clotting in human PPP. [1]
In rats and rhesus monkeys, activated partial throboplastin time was extended by dabigaran.
Rats orally administrated with dabigatran etexilate exerted anticoagulant effects in a dose and time –dependent manner. [1]
Compared with warfarin, dabigatran administered orally (150 mg dose) in patients with atrial fibraillation, exhibited lower rates of stroke and systemic embolism but similar rates of major hemorrhage. [2]
References:1. Wienen W, Stassen JM, Priepke H et al. In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62.2. Connolly SJ, Ezekowitz MD, Yusuf S et al. Dabigatran versus warfarin in patients with atrialfibrillation. N Engl J Med. 2009 Sep 17;361(12):1139-51.
