Dabigatran etexilate

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 Vitro):Dabigatran etexilate (BIBR 1048; 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 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 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 (BIBR 1048; 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 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 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-1048

Autophagy

Thrombin

Thrombin

Cardiovascular Disease

Thrombosis

211915-06-9

627.7332

C34H41N7O5

>98% (HPLC)

10 mM in DMSO

O=C(OCC)CCN(C1=NC=CC=C1)C(C2=CC=C3N(C)C(CNC4=CC=C(/C(N)=N\C(OCCCCCC)=O)C=C4)=NC3=C2)=O

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

(-20℃)

With Ice Pack

≥ 2 years