1. Metabolic Enzyme/Protease
  2. Thrombin
  3. Dabigatran

Dabigatran (Synonyms: BIBR 953; BIBR 953ZW)

Cat. No.: HY-10163 Purity: >98.0%
Handling Instructions

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

For research use only. We do not sell to patients.

Dabigatran Chemical Structure

Dabigatran Chemical Structure

CAS No. : 211914-51-1

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Based on 3 publication(s) in Google Scholar

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Description

Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=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]

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].

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].

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.
Clinical Trial
Molecular Weight

471.51

Formula

C₂₅H₂₅N₇O₃

CAS No.

211914-51-1

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
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
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: >98.0%

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Keywords:

DabigatranBIBR 953BIBR 953ZWBIBR953BIBR-953ThrombinInhibitorinhibitorinhibit

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