Dabigatran Etexilate Mesylate NEW
Price | $35 | $52 | $68 |
Package | 5mg | 10mg | 25mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-04 |
Product Details
Product Name: Dabigatran Etexilate Mesylate | CAS No.: 872728-81-9 |
Purity: 99.94% | Supply Ability: 10g |
Release date: 2024/11/04 |
Product Introduction
Bioactivity
名稱 | Dabigatran Etexilate Mesylate |
描述 | Dabigatran Etexilate Mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM). |
體外活性 | Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC50: 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 (IC50: 0.56 μM). 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 μM, respectively [1]. |
體內(nèi)活性 | 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 hemorrhages and hemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2]. |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 50 mg/mL (69.08 mM) |
關(guān)鍵字 | venousthromboembolism | prodrug | agent | anticoagulant | atrial | Dabigatran | fibrillation | orally | antithrombotic | Inhibitor | Thrombin | Dabigatran Etexilate Mesylate | effects | active | inhibit | Dabigatran etexilate |
相關(guān)產(chǎn)品 | (S)-(+)-Ibuprofen | Edoxaban | AEBSF hydrochloride | Heparin sodium salt | Thrombin (MW 37kDa) | Menadione | Ozagrel | Argatroban | Eltrombopag Olamine | p-Hydroxycinnamic acid |
相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | EMA 上市藥物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | FDA 上市藥物庫(kù) | 臨床期小分子藥物庫(kù) | 已知活性化合物庫(kù) | 抗COVID-19化合物庫(kù) | 凝血與抗凝化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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