factor xa (human)

Apixaban (BMS-562247-01) 是一种高度选择性，可逆的、口服具有活力的凝血因子 Xa (Factor Xa) 抑制剂，抑制人和兔凝血因子 Xa 的 Ki 分别为 0.08 nM 和 0.17 nM。它可以用于研究各种血栓栓塞疾病。

Zifaxaban (TY-602) 是一种具有口服活性、竞争性和选择性的 Xa 因子 (FXa) 抑制剂，对人 FXa 的 IC50 为 11.1 nM。Zifaxaban 的亲和力很高，比其他丝氨酸蛋白酶高 10000 倍以上。Zifaxaban 可用于研究动脉和静脉血栓形成。

Apixaban 13C,d3是Apixaban的氘代标记物，可用于同位素示踪。 是一种选择性的凝血因子 Xa (Factor Xa) 抑制剂，用于研究血栓栓塞。

O-Desmethyl apixaban is a metabolite of Apixaban and a highly selective, reversible inhibitor of Factor Xa, with Ki values of 0.08 nM in humans and 0.17 nM in rabbits.

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.

p-APMSF is an irreversible inhibitor of serine proteases with Ki values of 1.02, 1.18, 1.5, and 1.54 μM for bovine trypsin, human thrombin, bovine plasmin, and bovine Factor Xa, respectively. It is selective for these proteases over bovine chymotrypsin and acetylcholinesterase.

APC-6860 is a trypsin-like serine proteases inhibitor with k i values of 0.21, 0.44, 1.5, 16.8, 20, 30 μM for uPA, trypsin, tryptase, tPA, thrombin and factor Xa, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has k i values of 0.1, 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer.

Edoxaban (DU-176b) hydrochloride 是一种高效的、选择性的、口服具有活力的、直接的Factor Xa (FXa) 抑制剂，能够作用于人游离 FXa (Ki: 0.561 nM) 和凝血酶原酶 (Ki: 2.98 nM)。Edoxaban hydrochloride 的选择性是其他凝血蛋白酶的 10000 倍以上。Edoxaban hydrochloride 能够用于研究预防血栓栓塞性疾病。

Boc-Leu-Gly-Arg-AMC是一种特异性荧光底物，用于酶法检测和定量补体成分C3/C5转化酶、凝血因子Xa及大豆胰蛋白酶样酶活性。Boc-Leu-Gly-Arg-AMC还可被人红细胞分离的高分子量巯基蛋白酶——巨蛋白酶水解，使其成为酶学检测中的多功能工具。