spla2

KH064 is a sPLA2-IIA inhibitor of oral activity.

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.

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).

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.

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

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.

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.

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].

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.

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.

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.

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

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).

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

Scalaradial is an inhibitor of bee venom phospholipase A2 (PLA2) and TRPM ion channels (TRPM2) with IC50 values of 0.07 and 0.21 μM. It regulates ERK phosphorylation by inhibiting secretory PLA2 and Akt. Additionally, Scalaradial prevents the release of Arachidonic acid in mouse peritoneal macrophages induced by PMA.

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

Hnps-PLA Inhibitor is an inhibitor of human nonpancreatic secretory Phospholipase A (hnps-PLA).

GK241 (compound 31a-c), a 2-oxoamide-based compound, exhibits inhibitory activity against group IIA secretory phospholipase A2 (GIIA sPLA2) in humans and mice, with IC50 values of 143 nM and 68 nM, respectively. The mechanism of inhibition has been explored through molecular dynamics simulations.

secreted phospholipase A2 (sPLA2) inhibitor

Competitive inhibitor of secretory phospholipase A2 (sPLA2)

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

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