Dabigatran etexilate mesylate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BIBR-953 的前药，是一种有效的非肽凝血酶抑制剂，Ki 为 4.5 nM。

A prodrug of BIBR-953, which is a potent nonpeptide thrombin inhibitor with Ki of 4.5 nM; 10-fold less potent for Trypsin and no activity against Factor Xa, Plasmin, tPA and activated protein C; exhibits strong and long-lasting anticoagulant effects ex vivo and strong oral activity in different animal species.Thrombosis Approved(In Vivo):Dabigatran etexilate mesylate (BIBR 1048MS; oral; 10, 20 and 50 mg/kg for rats and 1, 2.5 and 5 mg/kg for monkeys) has dose- and time-dependent anticoagulant effects and has maximum effects between 30 and 120 min after administration, respectively.Dabigatran etexilate mesylate maximally and significantly prolongs partial thromboplastin time (aPTT) to 25.2, 38.4 and 78.3 s in 30 min after 10, 20 and 50 mg/kg oral doses, respectively.Dabigatran etexilate mesylate maximally prolongs the aPTT to 34.3 s, 44.0 s, and 63.0 s, respectively, 2h after 1, 2.5 or 5 mg/kg doses in the monkey.

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Dabigatran etexilate mesylate (BIBR 1048MS; oral; 10, 20 and 50 mg/kg for rats and 1, 2.5 and 5 mg/kg for monkeys) has dose- and time-dependent anticoagulant effects and has maximum effects between 30 and 120 min after administration, respectively. Dabigatran etexilate mesylate maximally and significantly prolongs partial thromboplastin time (aPTT) to 25.2, 38.4 and 78.3 s in 30 min after 10, 20 and 50 mg/kg oral doses, respectively.Dabigatran etexilate mesylate maximally prolongs the aPTT to 34.3 s, 44.0 s, and 63.0 s, respectively, 2h after 1, 2.5 or 5 mg/kg doses in the monkey. Animal Model:Male rats (280-350 g) and rhesus monkeys of either sex (3-8 kg) Dosage:10, 20 and 50 mg/kg for rats and 1, 2.5 and 5 mg/kg for monkeys Administration:Oral Result:Had dose- and time-dependent anticoagulant effects.

BIBR 1048MS | Dabigatran etexilate methanesulfonate

Autophagy

Thrombin

Thrombin-inducedplateletaggregation

Cardiovascular Disease

Thrombosis

872728-81-9

723.8389

C35H45N7O8S

>98% (HPLC)

10 mM in DMSO

O=C(OCC)CCN(C(C1=CC=C2C(N=C(CNC3=CC=C(C(NC(OCCCCCC)=O)=N)C=C3)N2C)=C1)=O)C4=NC=CC=C4.CS(=O)(O)=O

β-Alanine, N-[[2-[[[4-[[[(hexyloxy)carbonyl]amino]iminomethyl]phenyl]amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl]-N-2-pyridinyl-, ethyl ester, methanesulfonate (1:1)

(-20℃)

With Ice Pack

≥ 2 years