spla2

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

sPLA2 inhibitor 3 (Compound 6c) functions as a potent α-glucosidase inhibitor (IC50= 0.0953 µM) and has potential applications in diabetes research.

sPLA2 inhibitor 2 (compound 6a) is an sPLA2 inhibitor with an IC50 value of 0.0475 μM, making it valuable for diabetes research.

sPLA2-X Inhibitor 31 is a selective inhibitor of secreted phospholipase A2 type X (sPLA2-X) with IC50 values of 26 nM for sPLA2-X, 310 nM for sPLA2-IIa, and 2230 nM for sPLA2-V.

The sPLA2-IIA Inhibitor is a cyclic pentapeptide analog of FLSYK, specifically cyclic 2-Nal-Leu-Ser-2-Nal-Arg (c2), which interacts with human IIA phospholipase A2 (hGIIA) to impede its ester bond hydrolyzing function. As part of the esterase superfamily, sPLA2 enzymatically cleaves the sn-2 ester bond in glycerophospholipids, releasing arachidonic acid and lysophospholipids[1].

KH064 is a sPLA2-IIA inhibitor of oral activity.

Trimipramine maleate (Surmontil maleate) appears to inhibit serotonin transport and norepinephrine uptake by nerve terminals. This increases available norepinephrine or serotonin and prolongs its action. Trimipramine Maleate is the maleate salt form of trimipramine, a tricyclic secondary amine of the dibenzazepine class, with an antidepressant property.

Asenapine Maleate (Org 5222 maleate) is a second generation (atypical) antipsychotic agent that is taken sublingually and used in the treatment of schizophrenia and manic or mixed episodes associated with bipolar 1 disorder. Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury.

Varespladib (LY315920), a specific and effective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor(IC50=7 nM), has been investigated for the treatment and prevention of sickle cell disease, vaso-occlusive crisis, and acute coronary syndrome.

Tanshinone I (Tanshinone A), an active principle isolated from the herbal medicine Salvia miltiorrhiza, displays cytotoxicity against tumor cells.

RS-127445 hydrochloride (MT 500) is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist(pKi : 9.5).

Varespladib sodium (LY315920 sodium) is a highly potent and selective inhibitor of group IIA secretory phospholipase A2 (sPLA2), with an IC50 of 9 nM. It shows significant inhibitory activity against sPLA2 in serum samples from multiple species, including rat (IC50 of 8.1 nM), rabbit (IC50 of 5.0 nM), guinea pig (IC50 of 3.2 nM), and human (IC50 of 6.2 nM).

Phosphatidylethanolamines are important components of cell membranes and biochemical pathways of fatty acid synthesis. 1-Palmitoyl-2-linoleoyl PE (PLPE) is one of the many phosphatidylethanolamines that may be present in cellular membranes. It has been used in studies involving the biosynthesis of anandamide via the phospholipase A2 (PLA2) and lysoPLD pathways. PLPE can also be used as a specific substrate to assess the activity of sPLA2-IIA in the presence of other phospholipids.

Ochnaflavone is a natural product for research related to life sciences. The catalog number is TN5501 and the CAS number is 50276-96-5.

WAY-100635 maleate is a selective 5-hydroxytryptamine 1A receptor antagonist with an IC50 value of 0.91 nM and a Ki value of 0.39 nM. It is also a dopamine D4 receptor agonist with pIC50 values of 8.9 and 6.6 for 5-HT1A and α1-adrenergic, respectively.

Competitive inhibitor of secretory phospholipase A2 (sPLA2)

Asenapine hydrochloride (Org 5222 hydrochloride) is a 5-hydroxytryptamine receptor, adrenergic receptor, dopamine receptor and histamine receptor antagonist with antipsychotic effects used in neurological disorders such as schizophrenia and bipolar disorder.

FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM). It inhibits glucose-induced increases in prostaglandin E2 production and insulin secretion in human pancreatic islets when used at a concentration of 10 μM and inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2β in a concentration-dependent manner. FKGK 18 (20 mg/kg, 3 times per week) reduces blood glucose levels in an intraperitoneal glucose tolerance test, decreases the incidence of diabetes, and increases serum insulin levels in non-obese diabetic (NOD) mice.

Me-Indoxam is an inhibitor of sPLA2. It has no effect on arachidonic acid release and platelet activating factor synthesis.

Tris(2,4-di-tert-butylphenyl)phosphate (TDTBPP) isolated from Vitex negundoL inhibits secretory phospholipase A2 (sPLA2). Tris(2,4-di-tert-butylphenyl)phosphate has anti-inflammatory activity.

secreted phospholipase A2 (sPLA2) inhibitor

WAY-100635 Maleate is a specific and effective 5-HT receptor antagonist (IC50=0.95 nM).

Arachidonoyl Thio-PC is a substrate for various phospholipase A2s (PLA2s), including sPLA2, cPLA2, and iPLA2. Cleavage of the sn-2 fatty acid by PLA2 produces a free thiol that reacts with chromogenic reagents like DTNB (Ellman's reagent) and DTP, facilitating PLA2 activity quantitation. Isozyme-specific cPLA2 activity can be measured by excluding or inhibiting sPLA2 and iPLA2 activities in the assay.

Vilazodone D8 is a deuterium-labeled vilazodone. Vilazodone is a combined inhibitor of serotonin specific reuptake (SSRI) and agonist of 5-HT1A receptor partial.