thromboplastin

BMS-962212, a direct, reversible, and selective factor XIa (FXIa) inhibitor, demonstrates fast pharmacodynamic (PD) response onset and rapid elimination with a well-tolerated profile. It dependently increases activated partial thromboplastin time and decreases FXI clotting activity exposure [1].

FXIa-IN-15 (Compound (S)-10h) 是一种因子 XIa (FXIa) 和血浆激肽释放酶 (PKa) 的抑制剂，其 IC50 值分别为 0.38 nM 和 59.2 nM。FXIa-IN-15 具备抗凝特性，可以延长 50% 激活部分凝血活酶的时间 (aPTT)，其 EC1.5X 为 0.55 μM。

Thrombin inhibitor13 (Compound 13a) 是一种针对凝血酶 (thrombin, FIIa) 的共价可逆抑制剂，IC50为0.7 nM。Thrombin inhibitor13 能延长活化部分凝血活酶时间 (aPTT) 和凝血酶原时间 (PT)，显示出抗血栓和抗凝活性。

AZ12971554 is a potent inhibitor of human thrombin. Ki = 0.3nM, Activated partial thromboplastin time (APTT) IC50 = 0.68µM, Ecarin clotting time (ECT) IC50 = 0.16µM in human plasma.

JTV-803 is a factor Xa inhibitor. JTV-803 showed a competitive inhibitory effect on human factor Xa, with a K(i) value of 0.019 microM and IC(50) value of 0.081 microM. JTV-803 was 100 times more selective in inhibiting human factor Xa as compared to its

PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM). It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.

Dabigatran acyl-β-D-glucuronide is a major active metabolite of the thrombin inhibitor dabigatran . The prodrug of dabigatran, dabigatran etexilate , is hydrolyzed by plasma esterases to form dabigatran, which is metabolized primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT2B15 to form dabigatran acyl-β-D-glucuronide. Dabigatran acyl-β-D-glucuronide increases activated partial thromboplastin time (aPTT) in isolated human platelet-poor plasma equipotently to dabigatran.

Dabigatran acyl-β-D-glucuronide是凝血酶抑制剂dabigatran的一种活性代谢产物，主要通过UDP-葡萄糖醛酸转移酶(UGT)的UGT2B15亚型形成。在人体去除血小板的贫血浆中，Dabigatran acyl-β-D-glucuronide (0.46 µM) 能增加活化部分凝血活酶时间(aPTT)。