Dabigatran (BIBR 953) 211914-51-1

Molecular Weight: 471.51 Dabigatran (BIBR 953) is a Potent Nonpeptide Thrombin Inhibitor with an IC50 of 9.3 nM.


Biological Activity


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 μM, 3.8 μM, 50 nM, 45 μM and 20 μM, respectively. BIBR 953 specifically and reversibly inhibits thrombin.


BIBR 953 exhibits the most favorable activity profile following i.v. administration to rats. 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.


Protocol(Only for Reference)


Kinase Assay: [1]

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 μM -100 μM) 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	471.51
Formula	C25H25N7O3
CAS No.	211914-51-1

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	0.5 mg/mL (1.06 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (

Chemical Name	3-(2-((4-carbamimidoylphenylamino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoic acid

Contact us if you need more details on 211914-51-1. We are ready to answer your questions on packaging, logistics, certification or any other aspects about Dabigatran 211914-51-1、BIBR 953 211914-51-1. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : Others > Thrombin Inhibitor