VAP-1 Inhibitor

PXS-4728A is an orally active, selective VAP-1/SSAO inhibitor with an IC₅₀ of 5 nM and a K_i of 175 nM. PXS-4728A inhibits the expression of MMP-9. It reduces cell rolling, adhesion and migration, decreases cell infiltration levels, pro-inflammatory cytokines, chemokines and collagen deposition, and improves pulmonary function. PXS-4728A reduces the formation and progression of atherosclerotic plaques, and decreases blood lipid and blood glucose levels as well as body weight gain. PXS-4728A can be used in research related to chronic obstructive pulmonary disease, cystic fibrosis, acute pulmonary inflammation, acute lung injury, bronchiolitis obliterans syndrome, rhinovirus-exacerbated asthma, sepsis, Klebsiella pneumoniae pulmonary infection and atherosclerosis.

Semicarbazide hydrochloride is an orally active urea derivative. Semicarbazide hydrochloride binds to copper or iron in cells. Semicarbazide hydrochloride inhibits the activity of soluble semicarbazide sensitive amine oxidase (SSAO). Semicarbazide hydrochloride damages cartilage, blood vessels, ovaries, testicles, and thyroid follicles.

Mofegiline hydrochloride (MDL72974A) is an orally active and selective enzyme-activated irreversible inhibitor of MAO-B, with marked selectivity on the MAO-B over MAO-A with IC₅₀s of 3.6 nM (MAO-B) and 680 nM (MAO-A), respectively. Mofegiline hydrochloride is also an inhibitor of semicarbazide-sensitive amine oxidase (SSAO).

Semicarbazide-¹³C,¹⁵N₂ (Aminourea-¹³C,¹⁵N₂) hydrochloride is the ¹³C- and ¹⁵N-labeled Semicarbazide hydrochloride (HY-Y0470). Semicarbazide hydrochloride is an orally active urea derivative. Semicarbazide hydrochloride binds to copper or iron in cells. Semicarbazide hydrochloride inhibits the activity of soluble semicarbazide sensitive amine oxidase (SSAO). Semicarbazide hydrochloride damages cartilage, blood vessels, ovaries, testicles, and thyroid follicles.

Timolumab (BTT1023 ), a recombinant fully human monoclonal antibody that specifically binds VAP-1. Timolumab (BTT1023 ) could be used in the study of chronic inflammatory diseases.

Semicarbazide(hydrochloride (Standard) (Aminourea hydrochloride (Standard)) is the analytical standard of Semicarbazide hydrochloride (HY-Y0470). This product is intended for research and analytical applications. Semicarbazide hydrochloride is an orally active urea derivative. Semicarbazide hydrochloride binds to copper or iron in cells. Semicarbazide hydrochloride inhibits the activity of soluble semicarbazide sensitive amine oxidase (SSAO). Semicarbazide hydrochloride damages cartilage, blood vessels, ovaries, testicles, and thyroid follicles.

SSAO inhibitor-1 is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor. SSAO inhibitor-1 has anti-inflammatory activity and can be used for liver diseases research.

Vapaliximab (2D10) is a monoclonal antibody against human VAP-1.

PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a K_i of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects.

SNT-8370 is an orally active inhibitor of VAP-1 (IC₅₀: 10 nM) and myeloperoxidase (MPO) (IC₅₀: 17 nM), with >100-1000 fold more potency for VAP-1 and MPO versus other mammalian (per)oxidases. SNT-8370 inhibits MPO-mediated LDL lipid peroxidation. SNT-8370 inhibits leukocyte infiltration in lung injury models of acute inflammation. SNT-8370 is an anti-inflammatory agent, and can be used for research of inflammatory disorders.

VAP-1-IN-2 is an orally active VAP-1 inhibitor with an IC₅₀ value of 0.025 μM against human VAP-1 and 0.015 μM against rat VAP-1. VAP-1-IN-2 inhibits urinary protein excretion and the progression of proteinuria in diabetic rats. VAP-1-IN-2 inhibits VAP-1 activity in rats. VAP-1-IN-2 can be used in research related to diabetes and nephropathy.

LJP 1586 is an amine-based inhibitor of semicarbazide-sensitive amine oxidase (SSAO) activity. LJP 1586 is an orally active, potent and selective inhibitor of rodent and human SSAO activity, with IC₅₀ values between 4 and 43 nM.

SSAO inhibitor-2 is a selective semicarbazide-sensitive amine oxidase (SSAO/VAP-1) inhibitor with an IC₅₀ of < 10 nM. SSAO inhibitor-2 can be used for the research of inflammation diseases, diabetes and diabetes-related diseases, mental disorders, pain-related diseases, ischemic diseases, vascular diseases, ocular diseases, fibrosis, neuroinflammatory diseases, cancer, and tissue transplant rejection.

SSAO inhibitor-3 (Compound 2) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC₅₀s of <10 nM, and 0.1-10 μM for human SSAO and AOC1, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc.

MD 220661 is a semicarbazide-sensitive amine oxidase (SSAO) and monoamine oxidase (MAO) inhibitor, and serves as a major metabolite of MD 240928 in rat brain. MD 220661 acts as a substrate for SSAO and exhibits reversible, selective MAO-B inhibition in rat tissues; in the absence of semicarbazide, its inhibitory potency against MAO-A activity decreases with prolonged pre-incubation time. MD 220661 is applicable to studies related to enzyme-catalyzed metabolism.

VAP-1-IN-3 (compound 136) is a potent amine oxidase vascular adhesion protein-1 (VAP-1) inhibitor, with an IC₅₀ of 0.13 μM for VAP-1 isolated from bovine plasma. VAP-1-IN-3 can be used for the research of inflammatory.

SSAO/VAP-1 inhibitor 1 is a potent inhibitor of SSAO/VAP-1. SSAO/VAP-1 promotes the transfer of Glucose transport 4 (GLUT 4) from adipocytes to the cell membrane, thereby regulating glucose transport. In endothelial cells, SSAO/VAP-1 can mediate the adhesion and exudation of leukocytes and endothelial cells, and participate in inflammatory responses. SSAO/VAP-1 inhibitor 1 has the potential for the research of inflammation and/or inflammation-related disease or diabetes and/or diabetes-related disease (extracted from patent WO2021102774A1, compound E3).

PXS-4728A free base is an orally active, selective VAP-1/SSAO inhibitor with an IC₅₀ of 5 nM and a K_i of 175 nM. PXS-4728A free base inhibits the expression of MMP-9. It reduces cell rolling, adhesion and migration, decreases cell infiltration levels, pro-inflammatory cytokines, chemokines and collagen deposition, and improves pulmonary function. PXS-4728A free base reduces the formation and progression of atherosclerotic plaques, and decreases blood lipid and blood glucose levels as well as body weight gain. PXS-4728A free base can be used in research related to chronic obstructive pulmonary disease, cystic fibrosis, acute pulmonary inflammation, acute lung injury, bronchiolitis obliterans syndrome, rhinovirus-exacerbated asthma, sepsis, Klebsiella pneumoniae pulmonary infection and atherosclerosis.