pai1

GW-6604, an ALK5 inhibitor, exhibits clear antifibrotic effects leading to improved liver function.

Upamostat is an inhibitor of a serine protease and is a urokinase plasminogen activator (uPA) inhibitor.

Tiplaxtinin (Tiplasinin)(PAI-039) is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 uM.

AZ3976 is an inhibitor of PAI-1 with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 displays profibrinolytic activities.

Angstrom6 (A-6 peptide) is an 8 amino acid peptide derived from single chain urokinase fibrinogen activator (scuPA) that interferes with the uPA/uPAR cascade and abrogates the downstream effects.Angstrom6 has antitumor activity and inhibits tumor cell migration, invasion, and metastasis by binding to CD44 and modulating CD44-mediated cell signaling.

Aleplasinin (PAZ 417) is a selective and orally active inhibitor of Plasminogen activator inhibitor-1(PAI-1) and a key negative regulator of the fibrinolytic system. Aleplasinin can be used in Alzheimer's disease studies.

UK-371804 is an effective and specific uPA inhibitor. It was selected as a candidate for further preClinicalal evaluation for the treatment of chronic dermal ulcers.

Loureirin B can downregulate the expression of fibrosis-related molecules by regulating MMPs and TIMPs levels, inhibit scar fibroblast proliferation and suppress TGF-β1-induced fibrosis, during which TGF-β1/Smad2/3 pathway is likely involved.

TM5441 is an orally bioavailable fibrinogen activator inhibitor-1 inhibitor that inhibits several cancer cell lines with IC50 values ranging from 13.9 to 51.1 μM.It induces intrinsic cell death in several human cancer cells and attenuates Nω-nitro-1-arginine methyl ester-induced cardiac hypertension and vascular senescence.

TM5275 sodium is a bioactive oral inhibitor of PAI-1 (plasminogen activator inhibitor-1), with an IC50 value of 6.95 μM.

Toddalolactone ((+)-Toddalolactone) is an anti-inflammatory and analgesic.

TM5007 is a poent inhibitor of plasminogen activator inhibitor-1 (PAI-1; IC50 of 29 uM).

Flavanone (2-Phenylchroman-4-one)s from citrus fruits have also been shown to exert beneficial effects on human vascular function. In particular, chronic interventions with orange juice, or the pure flavanone hesperidin, resulted in a decrease in blood pressure in overweight volunteers and acute improvements in microvascular reactivity.

6-Aminocaproic acid (EACA) is an antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.

4-Aminobenzamidine dihydrochloride (p-Aminobenzamidine dihydrochloride) is a strong trypsin inhibitor and a relatively weak inhibitor of urokinase type plasminogen activator (uPA) (K i =82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice [1] [2].

Diaplasinin (PAI-749) is a highly efficient inhibitor of plasminogen activator inhibitor-1 (PAI-1) with antithrombotic activity. It can be used in cardiovascular disease research.

UKI-1 is a urokinase-type plasminogen activator system synthetic inhibitor.

ZK824190 is an orally available and selective inhibitor of urokinase plasminogen activator (uPA), with IC50 values of 237 nM for uPA, 1600 nM for tPA, and 1850 nM for Plasmin.

ZK824859 is an orally available and selective inhibitor of urokinase plasminogen activator (uPA) with IC50 values of 79 nM for human uPA, 1580 nM for tPA, and 1330 nM for plasmin.

Fendosal (HP-129) is a non-steroidal anti-inflammatory agent. It is 6.9 to 9.5 times more active than aspirin in the prophylactic and therapeutic adjuvant-induced polyarthritis models of chronic inflammation.

Muvalaplin tetrahydrochloride (LY3473329) is an orally active lipoprotein (a)Lp(a) agent currently under investigation. Research on the oral formulation of Muvalaplin tetrahydrochloride is ongoing.

PPACK is a synthetic peptide derivative. It also irreversibly and specifically inhibits thrombin-mediated platelet activation by binding with high affinity to the active site of thrombin (Ki = 0.24 nM).

Alpha 2 Antiplasmin serves as the principal circulating inhibitor of plasmin. This compound plays a crucial role in regulating fibrinolysis within blood vessels.

BT-114143 is a plasminogen activator inhibitor with an IC50 of 8.42 μM. It is applicable in research related to hemorrhagic diseases caused by excessive fibrinolysis, including traumatic bleeding, severe menorrhagia, postpartum hemorrhage, and complications of hemophilia.