Phospholipase Inhibitor

Lp-PLA2-IN-16 (example 1) is a lipoprotein-associated phospholipase A2 (Lp-PLA 2) inhibitor, which can be used in the research of Alzheimer's disease, etc.

DPTIP hydrochloride is a potent brain penetrant neutral sphingomyelinase 2 (N-SMase 2) inhibitor (exosome inhibitor), with an IC₅₀ of 30 nM.

(R)-Bromoenol lactone-d₇ ((R,E)-Bromoenol lactone-d₇) is the deuterated-labeled (R)-Bromoenol lactone (HY-117068). (R)-Bromoenol lactone ((R,E)-Bromoenol lactone) is an isomer of Bromoenol lactone (HY-107411). (R)-Bromoenol lactone acts as a selective inhibitor of microsomal calcium-independent phospholipase A2γ (iPLA2γ). (R)-Bromoenol lactone induces mild activation of p38 mitogen-activated protein kinase in prostate cancer cells, resulting in slight increases in the expressions of phosphorylated p53, total p53 and p21. (R)-Bromoenol lactone is applicable to prostate cancer-related research.

Fuzapladib calcium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib calcium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib calcium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site.

7,7-Dimethyl-(5Z,8Z)-eicosadienoic acid (DEDA), a phospholipase inhibitor, is a non-metabolizable analog of arachidonic or eicosadienoic acid. 7,7-Dimethyl-(5Z,8Z)-eicosadienoic acid (DEDA) inhibits P388D1 cell phospholipase A₂ (PLA₂) (IC₅₀ = 16 µM) and snake venom PLA₂ (IC₅₀ = 14 µM).

GK563 is a selective Ca²⁺-independent phospholipase A₂ (GVIA iPLA₂) inhibitor with an IC₅₀ value of 1 nM. GK563 is 22000 times more active against GVIA iPLA₂ than GIVA cPLA₂. GK563 reduces β-cell apoptosis induced by proinflammatory cytokines, raising the possibility that it can be beneficial in countering autoimmune diseases, such as type 1 diabetes.

U-26384 is a Phospholipase A₂ inhibitor. U-26384 reduces Sodium iodoacetate (HY-D0849)-induced Arachidonic acid (HY-109590) release and cell damage. U-26384 can be used for research on Graves' disease and ischemic brain injury.

RHC 80267 (Standard) is the analytical standard of RHC 80267 (HY-107416). This product is intended for research and analytical applications. RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC₅₀ of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC₅₀ of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).

CRM-51005 is a phospholipase C (PLC)γ1 inhibitor with a bovine IC₅₀ of 13.0 μg/mL. CRM-51005 inhibits PLCγ1 enzymatic activity and platelet-derived growth factor-induced phosphoinositide turnover. CRM-51005 acts as a cell growth inhibitor via suppression of PLC, phosphoinositide turnover, DNA synthesis, and cell proliferation.

LCL521 dihydrochloride (Standard) is the analytical standard of LCL521 dihydrochloride (HY-103593A). This product is intended for research and analytical applications. LCL521 dihydrochloride is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).

PLA2-IN-1 (Compound 7) is a potent and selective inhibitor of phospholipase A₂ (PLA₂) with an IC₅₀ value of 1 nM PLA2-IN-1 inhibits PLA₂-induced coagulopathy in vitro. PLA2-IN-1 is promising for research of snakebite envenomation caused by cobra venom.

Varespladib (sodium) (Standard) is the analytical standard of Varespladib (sodium). This product is intended for research and analytical applications. Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively.

ST271 (Standard) is the analytical standard of ST271 (HY-103097). This product is intended for research and analytical applications. ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC₅₀s of 6.7 and 9 μM, respectively.

ML349 (Standard) is the analytical standard of ML349 (HY-100737). This product is intended for research and analytical applications. ML349 is a potent and specific acyl protein thioesterase 2(APT2)/lysophospholipase 2 (LYPLA2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.

CGP-35949 sodium is a LTD4 antagonist with phospholipase inhibitory activity. CGP-35949 sodium can be used for research of asthma.

Cinatrin A has the activity of inhibiting phospholipase A2.

Magnesium sulfate heptahydrate, United States Pharmacopeia (USP) Reference Standard (Epsom salts (Pharmaceutical primary standard, USP)) is a reference standard for Magnesium sulfate (HY-Y1267). Magnesium sulfate is a calcium antagonist and a potent L-type calcium channel inhibitor, as well as a tocolytic. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in the research of diseases such as preeclampsia/eclampsia.

Rhamnetin (Standard) is the analytical standard of Rhamnetin. This product is intended for research and analytical applications. Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2 and histone deacetylase 2 (HDAC2). Rhamnetin exhibits antitumor, antioxidant and anti-inflammatory activity.

(R)-N-(1-Hydroxypropan-2-yl)palmitamide (compound 24) is a substrate analog inhibitor of phospholipase A2.

BAPTA tetrasodium (Standard) is the analytical standard of BAPTA tetrasodium. This product is intended for research and analytical applications. BAPTA tetrasodium is a selective and cell-impermeant chelator for calcium. BAPTA tetrasodium, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrasodium is widely used as an intracellular buffer for investigating the effects of Ca²⁺ release from intracellular stores or influx via Ca²⁺-permeable channels in the plasma membrane. BAPTA tetrasodium can also inhibit phospholipase C activity independently of their role as Ca²⁺ chelators.