达比加群 T6295

Product Introduction
Bioactivity


英文名: Dabigatran

描述: Dabigatran (BIBR 953ZW) 是一种口服抗凝剂，是一种可逆的，竞争性的直接凝血酶 (thrombin) 抑制剂，Ki=4.5 nM。它也抑制凝血酶诱导的血小板聚集 (IC50=10 nM)。

体外活性: 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. [1] BIBR 953 specifically and reversibly inhibits thrombin. [2]

体内活性: BIBR 953 exhibits the most favorable activity profile following i.v. administration to rats. [1] 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. [3]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: 0.1 M HCL : 12.5 mg/mL (26.51 mM)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 0.1 mg/mL (insoluble)


关键字: Inhibitor | Dabigatran | inhibit | BIBR953 | Thrombin | BIBR-953

相关产品: Enoxaparin sodium | Pirodomast | RS-601 | TFLLRNPNDK-NH2 | Thrombin receptor peptide ligand | Eltrombopag | (S)-(+)-Ibuprofen | Efegatran sulfate | p-Hydroxycinnamic acid | Dabigatran ethyl ester

相关库: Drug Repurposing Compound Library | Approved Drug Library | FDA-Approved & Pharmacopeia Drug Library | Clinical Compound Library | Coagulation and Anticoagulation Compound Library | Human Metabolite Library | Inhibitor Library | Pediatric Drug Library | Orally Active Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途