Dabigatran ethyl ester hydrochloride 是一种核糖基二氢烟酰胺脱氢酶抑制剂,IC50=0.8 μM,也是一种凝血酶的抑制剂。
产品描述
Dabigatran ethyl ester hydrochloride is an effective inhibitor of ribosyl dihydronicotinic acid amide dehydrogenase (NQO2) with an IC50 value of 0.8 μM and is a thrombin inhibitor.
体外活性
Dabigatran (ethyl ester hydrochloride) has a Ki of 0.9 μM for NQO2 and an IC50 of 0.8 μM. The ethyl group (ethyl ester hydrochloride) of dabigatran significantly extends the interaction surface, especially with hydrophobic amino acids (such as Ile 128 and Met 154). Dabigatran ethyl ester has a higher affinity for thrombin and NQO2 than dabigatran [1]. Dabigatran is a highly selective, reversible and effective thrombin inhibitor, which can be taken orally as a prodrug dabigatran etexilate .
体内活性
Dabigatran (Ki = 4.5 nM) can selectively bind to human thrombin and reversibly achieve a strong and lasting anticoagulant effect.
Cas No.
211914-50-0
分子式
C27H30ClN7O3
分子量
536.03
别名
N-[[2-[[[4-(氨基亚氨甲基)苯基]氨基]甲基]-1-甲基-1H-苯并咪唑-5-基]羰基]-N-(2-吡啶基)-BETA-丙氨酸乙酯盐酸盐
储存和溶解度
DMSO:50 mg/mL (93.28 mM)
H2O:5 mg/mL (9.33 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years