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Dabigatran etexilate mesylate (Synonyms: BIBR 1048MS)

Catalog No.GC15390 Copy One-Click Copy Product Info

A prodrug form of dabigatran

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Dabigatran etexilate mesylate Chemical Structure

Cas No.: 872728-81-9

Size Price Stock Qty
10mM (in 1mL DMSO)
$30.00
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5mg
$19.00
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10mg
$28.00
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50mg
$77.00
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100mg
$112.00
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200mg
$165.00
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500mg
$267.00
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1g
$392.00
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Sample solution is provided at 25 µL, 10mM.



Description of Dabigatran etexilate mesylate

Description: IC50 Value: 4.5nM (Ki); 10nM(Thrombin-induced platelet aggregation) [1] Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) undergoing advanced clinical development as its orally active prodrug,dabigatran etexilate. in vitro: Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated 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 PPP at concentrations of 0.23, 0.83 and 0.18 microM, respectively [1]. in vivo: Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial haemorrhages and haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2]. Clinical trial: An Evaluation of the Pharmacokinetics and Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1

Chemical Properties of Dabigatran etexilate mesylate

Cas No. 872728-81-9 SDF
Synonyms BIBR 1048MS
Chemical Name ethyl 3-(2-(((4-(N-((hexyloxy)carbonyl)carbamimidoyl)phenyl)amino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanoate methanesulfonate
Canonical SMILES CCCCCCOC(NC(C1=CC=C(NCC2=NC3=C(C=CC(C(N(C4=CC=CC=N4)CCC(OCC)=O)=O)=C3)N2C)C=C1)=N)=O.CS(=O)(O)=O
Formula C35H45N7O8S M.Wt 723.84
Solubility ≥ 36.192 mg/mL in DMSO, ≥ 45.8 mg/mL in EtOH with gentle warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Dabigatran etexilate mesylate

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1 mg 5 mg 10 mg
1 mM 1.3815 mL 6.9076 mL 13.8152 mL
5 mM 276.3 μL 1.3815 mL 2.763 mL
10 mM 138.2 μL 690.8 μL 1.3815 mL
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In vivo Formulation Calculator (Clear solution) of Dabigatran etexilate mesylate

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Review for Dabigatran etexilate mesylate

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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