Factor Xa Inhibitor

Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a K_i of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a K_i of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity.

ZK-813039 is a potent and orally active factor Xa inhibitor. ZK-813039 can prolong prothrombin time. ZK-813039 can be used for the research of cardiovascular disease.

FXIIa-IN-3 (Compound 8) is a potent and selective Factor XIIa (FXIIa) inhibitor, with an IC₅₀ of 0.045 μM. FXIIa-IN-3 also exhibits a substantial margin of selectivity against related serine proteases, including FXIa, FXa, and FIXa. FXIIa-IN-3 can be used for the research of thromboembolic diseases.

JTV-803 is a selective and competitive direct factor Xa (FXa) inhibitor with a K_i of 19 nM and an IC₅₀ of 81 nM against human FXa, and its action is independent of antithrombin III (ATIII). JTV-803 exhibits significantly higher selectivity for human FXa than for thrombin, plasmin, and trypsin. JTV-803 produces sustained ex vivo anti-FXa inhibitory activity in vivo. JTV-803 prolongs aPTT and PT, prevents dialyzer thrombosis, and is cleared during dialysis. JTV-803 dose-dependently attenuates coagulation activation, maintains plasma ATIII activity, reduces glomerular fibrin deposition, and improves survival rate. JTV-803 can be used for research related to thrombosis and hemodialysis anticoagulation.

Letaxaban (TAK-442) is an orally active and selective direct FXa inhibitor. Letaxaban is a drug with dual anticoagulant and anti-inflammatory activity that works by directly inhibiting FXa and by intervening in the PAR1 signaling pathway. Letaxaban can be used in the study of thrombotic diseases, cardiovascular diseases and inflammation-related diseases.

EMD 495235 is a potent and orally active coagulation factor Xa inhibitor with an IC₅₀ of 5.5 nM and a K_i of 6.8 nM. EMD 495235 shows anticoagulant activities.

Naroparcil is an orally active antithrombotic agent. Naroparcil exhibits antithrombotic effects in rabbit Wessler stasis model with EC₅₀s of 21.9 mg/kg and 36.0 mg/kg after respectively intravenous injection and oral administration.

FXIa-IN-16 is an orally active selective FXIa inhibitor with an IC₅₀ of 0.19 nM. FXIa-IN-16 exerts highly selective competitive inhibition on endogenous FXIa, blocks the thrombin amplification loop to inhibit thrombosis, while preserving exogenous physiological hemostatic function. FXIa-IN-16 can be used in thrombosis-related research.

Coumafuryl-d₃ is the deuterium labeled Coumafuryl (HY-121244). Coumafuryl is a kind of coumarin rodenticide. Coumafuryl inhibits the metabolic cycle of vitamin K that causes the interference with protein biosynthesis of vitamin K-dependent coagulant factors (II, VII, IX, and X factors) in the liver.

FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an K_i of 0.17 nM. FXIa-IN-10 has good oral bioavailability.

FAM labled Fitusiran sodiumis a FAM labled Fitusiran sodium (HY-132587A). Fitusiran (ALN-AT3SC) sodium is a siRNA strategy. Fitusiran delivers siRNA targeting the SERPINC1 gene in hepatocytes to inhibit antithrombin synthesis. Fitusiran sodium enhances thrombin activity and increases Thrombin generation, thereby restoring hemostatic function. Fitusiran sodium can be used in hemophilia-related research.

FXIa-IN-6 is a potent FXIa inhibitor with selectivity against most of the relevant serine proteases (K_i = 0.3 nM).

DX-9065a is a selective, nonpeptidic, and orally active factor Xa (FXa) inhibitor with a K_i of 41 nM for human FXa. DX-9065a has low activity against other serine proteases. DX-9065a has strong anticoagulant actions.

DPC423 is a selective and orally active factor Xa inhibitor with a K_is of 0.15 (human) and 0.3 (rabbit) nM. DPC423 exhibits K_is of 60, 61 and 6000 nM against human trypsin, plasma kallikrein and thrombin. DPC423 blocks the formation of prothrombinase complex, reduces thrombin production, inhibits fibrin formation and platelet activation. DPC423 can be used for the study of anticoagulation of arterial thrombosis.

Cy3 labled Fitusiran sodium is a Cy3 labled Fitusiran sodium (HY-132587A). Fitusiran (ALN-AT3SC) sodium is a siRNA strategy. Fitusiran delivers siRNA targeting the SERPINC1 gene in hepatocytes to inhibit antithrombin synthesis. Fitusiran sodium enhances thrombin activity and increases Thrombin generation, thereby restoring hemostatic function. Fitusiran sodium can be used in hemophilia-related research.

Anivamersen is an RNA aptamer to reverse the anticoagulant effect of the parenteral factor IXa inhibitor pegnivacogin. REG1 is a novel anticoagulation system consisting of pegnivacogin, an RNA aptamer inhibitor of coagulation factor IXa, and anivamersen, a complementary sequence reversal oligonucleotide.

LY-517717 is a potent and orally active FXa inhibitor. LY-517717 shows antithrombotic and anticoagulant activity. LY-517717 has the potential for the research of venous thromboembolism after hip or knee replacement.

BI-11634 is an orally active factor Xa inhibitor and a CYP3A4 substrate. The apparent K_m values for BI-11634 metabolism are 23 μM in human liver microsomes (HLMs) and 7.6 μM with recombinant CYP3A4. BI-11634 can be used for thromboembolic disease and CYP3A4-mediated drug metabolism research.

Pegnivacogin sodium is a novel RNA-aptamer based factor IXa inhibitor featuring a reversal agent, anivamersen.

Fondaparinux (sodium) (Standard) is the analytical standard of Fondaparinux (sodium). This product is intended for research and analytical applications. Fondaparinux sodium is an antithrombin-dependent factor Xa inhibitor.