Prostaglandin Receptor Inhibitor

EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC₅₀ of 10.5 μM. EIPA also enhances autophagy by inhibiting Na⁺/H⁺-exchanger 3 (NHE3). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.

Tranilast (MK-341) acts as an anti-atopic agent. Tranilast suppresses production of prostaglandin D2 (PGD2, IC₅₀= 0.1 mM). Tranilast sodium exhibits anti-inflammatory and immunomodulatory effects. Tranilast sodium antagonizes angiotensin II and inhibits its biological effects in vascular smooth muscle cells.

EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC₅₀ of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na⁺/H⁺-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.

Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC₅₀ values of 0.6±0.1 and 6.2±1.2 nM, respectively.

Cyanidin Chloride (IdB 1027) is an orally active antioxidant and enzyme inhibitor. Cyanidin Chloride has IC₅₀ values of 90 μM and 60 μM against PGHS-1 and PGHS-2, respectively. Cyanidin Chloride exhibits excellent antioxidant and anti-inflammatory activities, scavenges free radicals, inhibits lipid peroxidation, and protects DNA from cleavage. Cyanidin Chloride can be used in the research of inflammatory diseases.

L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice.

Ginsenoside Ro (Polysciasaponin P3; Chikusetsusaponin 5; Chikusetsusaponin V) exhibits a Ca²⁺-antagonistic antiplatelet effect with an IC₅₀ of 155 μM. Ginsenoside Ro reduces the production of TXA₂ more than it reduces the activities of COX-1 and TXAS.

NP-1815-PX sodium is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC₅₀ of 0.26 μM against human P2X4 receptors. NP-1815-PX sodium specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX sodium selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX sodium not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX sodium exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX sodium is used in studies related to asthma and inflammatory bowel disease (colitis).

Pectolinarin possesses anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin suppresses cell proliferation and inflammatory response and induces apoptosis via inactivation of the PI3K/Akt pathway.

Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C₄ (LTC₄), and prostaglandin D₂ (PGD₂).

Ozagrel (OKY-046) is a high selective and orally active thromboxane A₂ (TXA₂) synthase inhibitor with an IC₅₀ of 11 nM. Ozagrel exerts anti-platelet aggregation, vasodilation and anti-inflammatory effects by inhibiting the production of TXA₂ and increasing the production of prostacyclin (PGI2). Ozagrel can be used for the study of ischemic stroke, asthma and thromboembolic diseases.

Cornuside is an iridoid glycoside with anti-allergic, anti-inflammatory, and neuroprotective activities. Cornuside exerts anti-allergic activity by downregulating the p38 MAPK, JNK, and NF-κB signaling pathways, and inhibits IgE-mediated histamine release from mast cells. Cornuside improves cognitive impairment in mice by inhibiting BACE1 activity (IC₅₀ = 55.84 μg/mL) and enhancing ChAT activity. Cornuside inhibits LPS (HY-D1056)-induced inflammatory mediators, including iNOS, COX-2, PGE2, TNF-α, IL-6, and IL-1β, by suppressing NF-κB activation.

Triflusal is an orally bioavailable, blood-brain barrier-permeable dual Cyclooxygenase-1 (COX-1)/cAMP phosphodiesterase inhibitor. Triflusal inhibits platelet aggregation, NF-κB activation, iNOS activity, and prostaglandin synthesis in ischaemic tissue. Triflusal stimulates neutrophil nitric oxide production, eNOS protein expression, and cNOS activity. Triflusal alleviates cerebral ischemic injury in rats and ameliorates pathological lesions and related gene expression in transgenic Alzheimer’s disease models. Triflusal can be used for the research of thromboembolic/ischemic cardiovascular and cerebrovascular diseases, and Alzheimer’s disease.

Chondroitin sulfate (from chicken) (Chondroitin polysulfate (from chicken)) is an orally active, sulfated linear polysaccharide extracted from chickens, which belongs to glycosaminoglycans. Chondroitin sulfate (from chicken) reduces the phosphorylation levels of ERK1/2 and p38MAPK, inhibits the expression of inflammatory cytokines and MMP, and downregulates the levels of IL-1β, IL-6, TNF-α and PGE₂. Chondroitin sulfate (from chicken) improves motor function, protects cartilage tissue, reverses chondrocyte aggregation, and regulates the structure of intestinal flora. Chondroitin sulfate (from chicken) can be used in research related to osteoarthritis.

Ridogrel (R 68070) is an orally active combined thromboxane A2 synthetase inhibitor and thromboxane A2/prostaglandin endoperoxide receptor blocker. Ridogrel is potent antiplatelet agent. Anti-inflammatory activities.

Ascorbyl tetra-2-hexyldecanoate (tetra-isopalmitoyl Ascorbic acid; IPAA) is a lipophilic derivative of vitamin C (L-ascorbic acid). Ascorbyl tetra-2-hexyldecanoate (100 μM ) can prevent the decrease in viability of HaCaT keratinocytes induced by UVB, hydrogen peroxide, or tert-butyl hydroperoxide, and reduce the production of IL-1α and prostaglandin E2 (PGE2). Topical application of ascorbyl tetra-2-hexyldecanoate (1%) increases epidermal viability thickness, stratum corneum water content, and skin smoothness, and reduces skin roughness in hairless mice. Ascorbyl tetra-2-hexyldecanoate can be used to develop skin whitening agents in the beauty industry.

Ozagrel hydrochloride (OKY-046 hydrochloride) is a high selective and orally active thromboxane A₂ (TXA₂) synthase inhibitor with an IC₅₀ of 11 nM. Ozagrel hydrochloride exerts anti-platelet aggregation, vasodilation and anti-inflammatory effects by inhibiting the production of TXA₂ and increasing the production of prostacyclin (PGI2). Ozagrel hydrochloride can be used for the study of ischemic stroke, asthma and thromboembolic diseases.