mediator

Sphingosine-1-phosphate (S1P) is an agonist for S1P1-5 receptors and a ligand for GPR3, GPR6, and GPR12. As an intracellular second messenger, it mobilizes Ca2+ and acts as an extracellular ligand for G-protein coupled receptors. This important lipid mediator is generated from sphingosine or other membrane phospholipids.

PAF (C16) is a potent MAPK and MEK ERK activator that induces increased vascular permeability. PAF (C16) (PAF (C16)) is a platelet-activating factor, a phospholipid-derived mediator and a ligand for PAF G protein-coupled receptor (PAFR). PAF (C16) has shown anti-apoptotic and anti-inflammatory activity in vitro, inhibiting Caspase-dependent apoptosis by interacting with its receptor (PAF-R) to perform cell signaling.

Eclazolast (RHC 2871) is a lipophilic anti-allergic compound that inhibits mediator release in a mast cell model.Eclazolast inhibits extracellular secretion by affecting only the direct processes associated with Fc(epsilon)RI in the cell.The effect of Eclazolast is highly dependent on the concentration of antigen that triggers the cell.

Leukotriene C4 (LTC4) is an arachidonate lipid mediator that regulates leukocyte recruitment and function at sites of inflammation.Leukotriene C4 is a mediator of bronchoconstriction, mucus hypersecretion, and eosinophilia, and has a mediating role in urticaria.

Quazolast (RHC 3988) is a potent mediator release inhibitor used as a control against ragweed antigenic nasal challenge and demonstrates superiority over placebo in preventing nasal congestion and nasal itching following such challenges.

Leukotriene D4 (LTD4) is a potent pro-inflammatory mediator formed from arachidonic acid, a bronchoconstrictor, and induces osteoclast senescence.Leukotriene D4 induces transcriptional activity of potentially oncogenic genes and can be used in the study of asthma.

Salbutamol (Albuterol) stimulates beta2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of ATP to cyclic-3', 5'-adenosine monophosphate (cAMP). Salbutamol Sulfate is the sulfate salt of the short-acting sympathomimetic agent albuterol, a 1:1 racemic mixture of (R)-albuterol and (S)-albuterol with bronchodilator activity. Increased cAMP concentrations relax the bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. To a lesser extent, Salbutamol stimulates beta1-adrenergic receptors, thereby increasing the force and rate of myocardial contraction.

PTZ-343 is a potent enhancer of Luminol, acting as an electron transfer mediator. It reacts with HRP-II to release HRP and a PTZ-343 radical, which then oxidizes luminol anions to induce light emission.

Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders.

Sodium Hydrogen Sulfide (hydrate) is, like nitric oxide, an important gaseous mediator that has significant effects on the immunological, neurological, cardiovascular and pulmonary systems of mammals. Sodium Hydrogen Sulfide (hydrate) is an H2S donor commonly used in cellular and whole animal experimental systems. For example, it has been used to suggest that H2S promotes neutrophil migration, reduces airway inflammation, and protects neurites, heart, and intestine from chemical or ischemic-reperfusion damage.

3-Aminobenzamide (PARP-IN-1) is a potent PARP inhibitor (IC50 < 50 nM in CHO cells) and mediates oxidant-induced myocyte dysfunction during reperfusion.

Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

Saclofen is a sulfonic analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that acts as a competitive antagonist of the GABAB receptor (IC50: 7.8 μM).1 This compound can be used to determine the functional roles for the GABAB receptor as

Bradykinin is an inflammatory mediator. It is a peptide that causes blood vessels to dilate (enlarge) via the release of prostacyclin, nitric oxide, and Endothelium-Derived Hyperpolarizing Factor. Bradykinin is a physiologically and pharmacologically active peptide of the kinin group of proteins, consisting of nine amino acids.

CP-380736 (PF-00520893) is an epidermal growth factor receptor (EGFR) inhibitor. EGFR is a tyrosine kinase that activates MAPK, JNK, and Akt pathways, and is an important mediator of several types of cancer.

RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein.

SP 600125, negative control is a methylated analog of SP 600125 and can be used as a negative control for SP 600125. SP 600125, negative control inhibits DTP3 and GADD45β MKK7 (growth arrest and DNA damage-inducible β mediator-activated protein kinase kinase kinase 7) and is capable of restoring activation.The IC50s of SP 600125, negative control against JNK2 and JNK3 were 18 and 24 μM, respectively.

CI-949 is an allergic mediator release inhibitor that inhibits the release of leukotriene C4 D4 (LTC4 LTD4), histamine, and thromboxane B2 (TXB2) with IC50 values of 0.5 μM, 11.4 μM, and 0.1 μM, respectively.

GSK-5498A is a selective blocker of CARC (IC50, 1 μM). It inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.

Resolvin D2 (RvD2) is a potent TRPV1 inhibitor and pro-absorptive mediator with anti-inflammatory, anti-infective and pro-absorptive effects for the study of immune disorders and cancer.

Resolvin D1 (RvD1) is an endogenous pro-inflammatory mediator that blocks pro-inflammatory neutrophil migration by regulating actin polymerization, reduces TNF-α-mediated inflammation in macrophages, and enhances macrophage phagocytosis of apoptotic cells.

BI605906 is an IKKβ inhibitor that inhibits tumor necrosis factor alpha-dependent IkappaB degradation and expression of the pro-inflammatory mediator interleukin-6, which can be used to study inflammatory skin diseases such as psoriasis.

CLZ-8 (Mcl1-IN-8) is an orally active inhibitor of Mcl-1-PUMA (p53 up-regulated mediator of apoptosis) with radioprotective properties.CLZ-8 ameliorates radiation-induced HUVEC cell damage and reduces apoptosis counts, and inhibits radiation-induced overexpression of PUMA.

Resolvin E1 is an effective endogenous pro-resolving mediator of inflammation. Resolvin E1 has unique counterregulatory actions that inhibit PMN transendothelial migration. Resolvin E1 also acts as an effective inhibitor of leukocyte infiltration, dendrit