activated

Protease-Activated Receptor-4 diTFA,2454 is the proteinase-activated receptor-4 (PAR4)agonist

Activated Protein C (390-404), human acetate (Activated Protein C ) inhibits APC anticoagulant activity.

Protease-Activated Receptor-1, PAR-1 Agonist acetate is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist acetate corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].

Protease-Activated Receptor-2, amide (SLIGKV-NH2) is an agonist of PAR2 with an IC50 of 10.4 M.

Protease-Activated Receptor-1 Antagonist 2 is an orally active antagonist of protease-activated receptor-1 (PAR-1), demonstrating significant potency with an IC 50 of 7 nM. It exhibits favorable pharmacokinetic characteristics, making it valuable in cardiovascular disease (CVD) research, including studies on atherosclerosis and restenosis [1].

Protease-Activated Receptor-4 (PAR4) is a proteinase-activated receptor-4 agonist used in antiplatelet therapy.

Activated Protein C (390-404), human, a peptide derived from the vitamin K-dependent serine protease, effectively suppresses the anticoagulant activity of APC [1].

Protease-Activated Receptor-1 (PAR-1) Agonist TFA is a selective peptide that acts as an agonist for the proteinase-activated receptor-1 (PAR-1). Corresponding to the tethered ligand of PAR-1, this compound mimics the actions of thrombin through the PAR-1 receptor[1][2].

Activated EG3 Tail facilitates the synthesis of exon-skipping oligomer conjugates that target specific sites within the human anti-muscular atrophy protein gene, promoting exon 51 skipping. This compound holds potential for research into muscular dystrophy treatments [1].

Activated C Subunit is utilized in synthesizing exon jumping oligomer conjugates that complement specific target sites within the human anti-muscular atrophy protein gene to promote exon 51 skipping, offering a research avenue for muscular dystrophy [1].

Mitogen-activated protein kinase 1 (MAPK1) activates the p38 NF-κB pathway and regulates cellular processes in sepsis-associated diseases. Its catalytic action phosphorylates substrate proteins, serving as a regulatory switch for their activity [1].

TFRGAP-amide, human PAR-3-derived tethered ligand sequence which does not activate PAR-3 but rather activates PAR-1 and PAR-2, either in Jurkat or in other PAR-expressing cells.

Protease-Activated Receptor-1 antagonist 1 (Compound 13), a PAR-1 antagonist with an IC50 of 3 nM obtained by the FLIPR technique, can be used to study thrombotic cardiovascular diseases, myocardial infarction, and peripheral arterial disease.

Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA, is a peptide that acts as an agonist for the proteinase-activated receptor (PAR-3) [1].

Protease-Activated Receptor-1 antagonist 2 is a selective, orally active PAR-1 antagonist (IC50: 7 nM) with favorable pharmacokinetic properties, suitable for cardiovascular disease (CVD) research such as atherosclerosis and restenosis studies.

Drotrecogin alfa (activated) (DrotAA), a recombinant human activated protein C (APC), mitigates smoke-induced elevations in pulmonary microvascular permeability and proinflammatory cytokine IL-1β levels in rats. It also inhibits coagulation and inflammation while enhancing fibrinolysis. Drotrecogin alfa (activated) is applicable in severe sepsis research [1] [2].

Activated T Subunit is employed in synthesizing exon-jumping oligomer conjugates that target specific sites within the human anti-muscular atrophy protein gene to induce exon 51 skipping, a potential avenue for muscular dystrophy research [1].

Protease-Activated Receptor-1 antagonist 3 is a potent antagonist of Protease-Activated Receptor-1 (IC50: 7 nM) and exhibits binding affinity to hERG K+ channels (IC50: 9 μM).

The peptide region containing residues 390-404 in Activated Protein C (APC) is essential for anticoagulant activity and is available for interaction with antibodies or with other proteins, such as the macromolecular substrates Factors Va or VIIIa. APC reg

Activated DPG subunit facilitates the synthesis of exon jumping oligomer conjugates targeting specific sites within the human anti-muscular atrophy protein gene to induce exon 51 skipping, a potential research avenue for muscular dystrophy [1].

Activated A Subunit is instrumental in synthesizing exon skipping oligomer conjugates, which are designed to specifically pair with chosen sequences within the human anti-muscular atrophy protein gene, thereby promoting exon 51 skipping. This application is significant for research into muscular dystrophy [1].

Protease-Activated Receptor-1 (PAR-1) Agonist, a selective peptide, activates the PAR-1 receptor by mimicking the specific actions of thrombin. It corresponds to the PAR1 tethered ligand, facilitating selective activation of this receptor.

PAR-2 Activating Peptide acetate (SLIGRL-NH2 acetate) is an agonist of Protease-Activated Receptor-2 (PAR-2).

SLIGRL-NH2 TFA, also known as Protease-Activated Receptor-2 Activating Peptide TFA, is a Protease-Activated Receptor-2 (PAR-2) agonist [1].

SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is a PAR-2 agonist that induces non-histaminergic pruritus.

Z-VAD-FMK (Caspase Inhibitor VI) is a broad-spectrum inhibitor of caspases.Z-VAD-FMK binds to activated caspases and inhibits apoptosis.Z-VAD-FMK does not inhibit UCHL1 activity, even at concentrations up to 440 μM.

Lanifibranor (IVA337) is an agonist of peroxisome proliferator-activated receptors (PPARs) with EC50 values of 1,537, 866, and 206 nM for human recombinant PPARα, PPARβ, and PPARγ, respectively, for transactivation activity

Trastuzumab deruxtecan (T-DXd) is an antibody-activated molecule coupling (ADC) with anticancer and antitumour activity.Trastuzumab deruxtecan has been shown to have an ameliorative effect in HER2-positive breast and gastric cancers.

Clofibrate (Clofibrato) is an aryloxyisobutyric acid derivate with antihyperlipidemic activity.

Flufenamic acid (Arlef) is an anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically.

Palmitoylethanolamide (Impulsin) is an endogenously fatty acid amide. It has a role as an anti-inflammatory drug, an antihypertensive agent, a neuroprotective agent and an anticonvulsant.Upon administration, palmitoylethanolamide may inhibit the release of pro-inflammatory mediators from activated mast cells.

Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).

Methyl cinnamate, a tyrosinase inhibitor and a flavoring compound, has antimicrobial, antiadipogenic, vasorelaxant, and anti-inflammatory effects.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to and blocks activated (open) voltage-gated sodium channels, thereby blocks the influx of sodium ions into the cell, which leads to an increase in threshold for excitation and inhibit depolarization during phase 0 of the action potential.

Rosiglitazone maleate (BRL 49653) is the maleate salt of rosiglitazone, an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity.

Tetradecylthioacetic acid is a synthetic fatty acid with a sulfur substitution in the β-position. This modification renders TTA unable to undergo complete β-oxidation and increases its biological activity, including activation of peroxisome proliferator activated receptors (PPARs) with preference for PPARα.

Glabridin (KB-289522) may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-glucose levels; may possess a therapeutic effect on metabolic disorders( such as diabetes and hyperglycemia), by modulating glucose metabolism through AMPK in skeletal muscle cells. Glabridin may have potential as a chemopreventive agent against liver Y metastasis, by inhibiting the invasion of human HCC cells.

Daidzein (Isoflavone) is an isoflavone extract from soy, which is an inactive analog of the tyrosine kinase inhibitor genistein. It has antioxidant and phytoestrogenic properties.

Ifosfamide (NSC-109724) alkylates and forms DNA crosslinks, thereby preventing DNA strand separation and DNA replication. Ifosfamide is a synthetic analog of the nitrogen mustard cyclophosphamide with antineoplastic activity. This agent is a prodrug that must be activated through hydroxylation by hepatic microsomal enzymes.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

AICAR (Acadesine) is an AMPK activator that causes ZMP accumulation, thereby mimicking the stimulatory effect of AMP on both AMPK and AMPKK. It is commonly used in research related to diabetes, cardiovascular diseases, and tumors.

Lidocaine hydrochloride (Lignocaine hydrochloride) is a local anesthetic and cardiac depressant used as an antiarrhythmic agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.

Caffeic Acid Phenethyl Ester (Phenylethyl Caffeate) (CAPE) inhibits the activation of nuclear transcription factor NF-kappa B and may suppress p70S6K and Akt-driven signaling pathways, with antineoplastic, cytoprotective and immunomodulating activities. CAPE is the phenethyl alcohol ester of caffeic acid and a bioactive component of honeybee hive propolis. In addition, CAPE inhibits PDGF-induced proliferation of vascular smooth muscle cells through the activation of p38 mitogen-activated protein kinase (MAPK) and hypoxia-inducible factor (HIF)-1alpha and subsequent induction of heme oxygenase-1 (HO-1).

N,N'-Dimethylthiourea (DMTU) (DMTU), isolated from Allii Sativi Bulbus, is an orally active scavenger of hydroxyl radical ( OH) and blocks OH production by activated neutrophils in vitro. N,N'-Dimethylthiourea protects against water-immersion restraint stress (WIRS)-induced gastric mucosal lesions in rats by exerting its antioxidant action including OH scavenging and anti-inflammatory action [1][2] .

Buformin hydrochloride (NSC-528218) is a potent AMPK activator,an oral antidiabetic drug of the biguanide class. Buformin delays the absorption of glucose from the gastrointestinal tract increases insulin sensitivity and glucose uptake into cells and inhibits synthesis of glucose by the liver. Biguanides may antagonize the action of glucagon, thus reducing fasting glucose levels.

Cloxiquine (Dermofongin) is a monohalogenated 8-hydroxyquinoline with activity against bacteria, fungi, and protozoa.

Ciprofibrate (Win35833) is a fibrate derivative with antilipidemic activity.

Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx.

NPC 15199 (FMOC-L-Leucine) is an anti-inflammatory agent.