Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

Dabigatran [211914-51-1]

Stampa

Cat# HY-10163-10mg

Size : 10mg

Marca : MedChemExpress

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Description

Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (K_i=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC₅₀=10 nM)^[1]^[2].

IC₅₀ & Target

Ki: 4.5 nM (thrombin)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	25.3 μM Compound: Dabigatran	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	4.7 μM Compound: Dabigatran	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	8.1 μM Compound: Dabigatran	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
Platelet	EC₅₀	0.007 μM Compound: Dabigatran	Inhibition of thrombin induced platelet activation in CD-1 mouse plasma incubated for 2 mins by luminescence based assay Inhibition of thrombin induced platelet activation in CD-1 mouse plasma incubated for 2 mins by luminescence based assay	[PMID: 36462436]
Platelet	EC₅₀	0.029 μM Compound: Dabigatran	Inhibition of tissue factor induced platelet activation in 76% human blood incubated for 15 mins by CD62 antibody based assay Inhibition of tissue factor induced platelet activation in 76% human blood incubated for 15 mins by CD62 antibody based assay	[PMID: 36462436]
Platelet	IC₅₀	0.6 μM Compound: Dabigatran	Anticoagulant activity in mouse plasma assessed inhibition of thrombin-induced platelet aggregation Anticoagulant activity in mouse plasma assessed inhibition of thrombin-induced platelet aggregation	[PMID: 34902735]

In Vitro

Dabigatran (BIBR 953) shows concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human platelet-poor plasma at concentrations of 0.23, 0.83 and 0.18 μM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Dabigatran (0.01-0.1 mg/kg; i.v.) inhibits clot formation with an ED₅₀ of 0.033 mg/kg in Wessler model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male rats (Wessler model)^[3]
Dosage:	0.01, 0.03, 0.05 and 0.1 mg/kg
Administration:	Intravenous injection
Result:	Inhibited clot formation with an ED₅₀ of 0.033 mg/kg.

Essai clinique

Masse moléculaire

471.51

Formule

C₂₅H₂₅N₇O₃

CAS No.

211914-51-1

Appearance

Solid

Color

White to light yellow

SMILES

N=C(N)C(C=C1)=CC=C1NCC2=NC3=CC(C(N(CCC(O)=O)C4=NC=CC=C4)=O)=CC=C3N2C

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

0.1 M HCl : 12.5 mg/mL (26.51 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1208 mL	10.6042 mL	21.2085 mL
5 mM	0.4242 mL	2.1208 mL	4.2417 mL
10 mM	0.2121 mL	1.0604 mL	2.1208 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité
Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Pureté et documentation

Purity: 98.06%

Fiche technique (272 KB) SDS (393 KB)

COA (246 KB) RP-HPLC (227 KB) MS (205 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Wienen W, Stassen JM, Priepke H, In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally activeprodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62. [Content Brief]

[2]. Hauel NH, et al. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem. 2002 Apr 25;45(9):1757-66. [Content Brief]

[3]. Wienen W, et al. Effects of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate, on thrombus formation and bleeding time in rats. Thromb Haemost. 2007 Aug;98(2):333-8. [Content Brief]

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Dabigatran [211914-51-1]

Cat# HY-10163-10mg

Marca : MedChemExpress

Dabigatran Related Antibodies

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