Dabigatran

ArtNr	S2196-50
Hersteller	Selleckchem
CAS-Nr.	211914-51-1
Menge	50 mg
Quantity options	10 mg 1 g 10 g 200 mg 5 mg 50 mg 5 g
Kategorie	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Breast Cancer
Typ	Inhibitors
Specific against	other
Smiles	CN1C2=C(C=C(C=C2)C(=O)N(CCC(=O)O)C3=CC=CC=N3)N=C1CNC4=CC=C(C=C4)C(=N)N
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	BIBR 953
Similar products	BIBR
Lieferbar
Storage Conditions	2 years -80 in solvent
Molecular Weight	471, 51
Administration	Administered via i.v.
Animal Models	Rats
Clinical Trials	Dabigatran has entered in a phase III clinical trial in the treatment of atrial fibrillation.
IC50	9.3 nM [1], 9.3 nM [1], 9.3 nM [1], 9.3 nM [1], 9.3 nM [1], 9.3 nM [1]
In vitro	BIBR 953 is a very potent anticoagulant. BIBR 953 shows that the terminal phenyl can be substituted by the more hydrophilic 2-pyridyl group without substantial loss of activity. BIBR 953 inhibits thrombin, plasmin, factor Xa, trypsin, tPA and activated protein C with Ki of 4.5 nM, 1.7 uM, 3.8 uM, 50 nM, 45 uM and 20 uM, respectively. [1] BIBR 953 specifically and reversibly inhibits thrombin. [2]
In vivo	BIBR 953 exhibits the most favorable activity profile following i.v. administration to rats. [1] The bioavailability of dabigatran after p.o. administration of dabigatran etexilate is 7.2%. Dabigatran is predominantly excreted in the feces after p.o. treatment and in the urine after i.v. treatment. The mean terminal half-life of dabigatran is approximately 8 hours. Dabigatran acylglucuronides accounts for 0.4% and 4% of the dose in urine after p.o. and i.v. dosing, respectively. [3]
Kinase Assay	Measurement of thrombin inhibition, The thrombin inhibitory effects (IC50) of BIBR 953 is determined with a commercially available chromogenic assay. Human thrombin (0.042 U/mL) is preincubated for 10 minutes at 37 C with 10 different dilutions (concentration range of 0.003 uM -100 uM) of BIBR 953 dissolved in DMSO or with DMSO as control. Upon addition of the preincubation mixture to the chromogenic substrate, tosyl-glycyl-prolyl-arginine-4-nitranilide acetate, nitraniline is cleaved by thrombin and the increase in absorbance at 405 nm, related to the free nitraniline, is measured in a spectrophotometer. By plotting the absorbance at 405 nm vs the concentration of BIBR 953, the concentration that induces a 50% thrombin inhibition (IC50) is calculated. All measurements are performed in duplicate, and the mean values of both determinations are represented.
Solubility (25C)	DMSO <1 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	Dabigatran is a potent nonpeptide thrombin inhibitor with an IC50 of 9.3 nM in a cell-free assay.
Chemical Name	3-(2-((4-carbamimidoylphenylamino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoic acid
Features	Dabigatran is a reversible, competitive, direct thrombin inhibitor.

Hinweis: Die dargestellten Informationen und Dokumente (Bedienungsanleitung, Produktdatenblatt, Sicherheitsdatenblatt und Analysezertifikat) entsprechen unserem letzten Update und sollten lediglich der Orientierung dienen. Wir übernehmen keine Garantie für die Aktualität. Für spezifische Anforderungen bitten wir Sie, uns eine Anfrage zu stellen.

Alle Produkte sind nur für Forschungszwecke bestimmt. Nicht für den menschlichen, tierärztlichen oder therapeutischen Gebrauch.

Arbeitsanleitung (Data Sheet) anfordern

S2196-50-datasheet.pdf

S2196-50-safety-datasheet.pdf