PGE synthase Inhibitor

Zomepirac (McN-2783-21-98 free acid) is an orally active prostaglandin synthetase inhibitor. Zomepirac blocks prostaglandin synthesis and inhibits Collagen (HY-P72147)- or Epinephrine (HY-B0447)-induced platelet aggregation. Zomepirac can be used for the research of postoperative pain and osteoarthritis.

Fagaramide is a compound extracted from Zanthoxylum bungeanum with anti-inflammatory activity. It is effective against carrageenan foot swelling in rats and mediates its anti-inflammatory effect partly by inhibiting prostaglandin synthesis. Its activity is about 1/20 of that of indomethacin.

Cryogenine is an alkaloid originally isolated from H. salicifolia that has anti-inflammatory activity. It inhibits prostaglandin synthetase (IC₅₀=424 μM). Cryogenine (100 mg/kg per day, p.o.) reduces paw edema and the mean arthritic index in a rat model of adjuvant-induced polyarthritis.

LY3023703 is an orally active microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor. LY3023703 inhibits the production of PGE₂. LY3023703 is applicable to research related to inflammatory diseases and osteoarthritis pain.

15-PGDH-IN-5 is a sulfoxide-based inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH). 15-PGDH-IN-5 exhibits great water solubility, metabolic stability, and in vivo exposure levels. 15-PGDH-IN-5 blocks the 15-PGDH-mediated irreversible oxidative degradation of PGE2 and increases the effective concentration of endogenous PGE2 in tissues, thereby exerting anti-inflammatory effects and promoting tissue repair and regeneration. 15-PGDH-IN-5 is suitable for research into tissue injury and fibrosis-related diseases, such as inflammatory bowel disease and idiopathic pulmonary fibrosis.

Cafestol (Standard) is the analytical standard of Cafestol. This product is intended for research and analytical applications. Cafestol is an orally active diterpenoid and an inhibitor of ERK2. Cafestol has elevated blood lipids, anti-inflammatory, anti-angiogenic and anti-diabetic activities. In addition, Cafestol induces tumor cell apoptosis and autophagy, which can be used in the study of cancer.

5-trans U-46619 is a PGE synthase inhibitor. At a concentration of 10 μM, 5-trans U-46619 inhibits PGE synthase by <20%.

1-(2,5-Dihydroxyphenyl)-3-hydroxybutan-1-one is an inhibitor of iNOS and COX-2. 1-(2,5-Dihydroxyphenyl)-3-hydroxybutan-1-one inhibits LPS-induced excessive production of NO and PGE₂, as well as the mRNA expression of pro-inflammatory cytokines TNF-α, IL-1β, IL-6 and IL-12. 1-(2,5-Dihydroxyphenyl)-3-hydroxybutan-1-one can be used in inflammation-related research.

Ethyl Caffeate is a natural phenolic compound isolated from Bidens pilosa. Ethyl caffeate suppresses NF-κB activation and its downstream inflammatory mediators, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and prostaglandin E2 (PGE2) in vitro or in mouse skin.

Suprofen L-lysine (TN-762) is a non-steroidal anti-inflammatory drug (NSAID).

Dehydroevodiamine Standard is the analytical standard of Dehydroevodiamine (HY-N2106). This product is intended for research and analytical applications. Dehydroevodiamine is a blood-brain barrier-permeable, orally effective AChE and BACE1 inhibitor (IC₅₀ = 40.96 μM). Dehydroevodiamine is isolated and extracted from Evodia rutaecarpa. Dehydroevodiamine attenuates neurotoxicity through multiple targets by inhibiting BACE1 to block Aβ production, inhibiting AChE activity, scavenging ROS, and suppressing calcium influx. Dehydroevodiamine can be used for research on Alzheimer's disease, cerebral ischemia, vascular dementia, and other cognitive disorder-related diseases.

HPGDS inhibitor 1 (Standard) is the analytical standard of HPGDS inhibitor 1 (HY-10439). This product is intended for research and analytical applications. HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC₅₀s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.

Indigoticoside A is a phenylpropanoid lignan natural product that can be found in the traditional Chinese medicine Banlangen (Isatis indigotica Fort.), with antioxidant and anti-inflammatory activities. Indigoticoside A scavenges DPPH free radicals, superoxide anions and hydroxyl radicals in a dose-dependent manner, exhibiting significant in vitro antioxidant effects. The blood-absorbed components of Banlangen containing Indigoticoside A inhibit LPS (HY-D1056)-induced inflammatory responses in macrophages and reduce the production of inflammatory mediators such as NO, PGE₂ and TNF-α.

mPGES1-IN-3 is a selective, orally active mPGES-1 inhibitor with an IC₅₀ of 8.0 nM for h-mPGES-1 and an IC₅₀ of 10.79 nM for guinea pig mPGES1. mPGES1-IN-3 blocks the conversion of PGH2 (HY-136500) to PGE2 (HY-101952). mPGES1-IN-3 exhibits dose-dependent inhibition of LPS-induced thermal hyperalgesia. mPGES1-IN-3 can be used for research on rheumatoid arthritis.

Pratol (7-Hydroxy-4'-methoxyflavone) is an NF-κB inhibitor. Pratol also inhibits NO, PGE₂, TNF-α, IL-1β, and IL-6 production. Pratol increases the phosphorylation of p38 MAPK, JNK, and ERK, decreases AKT phosphorylation, and upregulates MITF, tyrosinase, TRP-1, and TRP-2 through a PKA-dependent signaling pathway. Pratol reduces iNOS and COX-2 protein expression, inhibits p65 phosphorylation, and protects IκBα from degradation, thereby inhibiting NF-κB nuclear translocation. Pratol can be used in research on hypopigmentary disorders, inflammatory diseases, cervical cancer, and colon cancer.

α-Gracinoic acid is an mPGES-1 inhibitor with anti-inflammatory activity.

F092 is an inhibitor of hematopoietic prostaglandin D synthase (H-PGDS) with a K_D value of 0.14 nM. F092 can be used in the study of allergic and inflammatory responses.

FR20 acts as an inhibitor of human microsomal prostaglandin synthase 1 (mPGES 1).

Zomepirac sodium salt (Standard) is the analytical standard of Zomepirac sodium salt (HY-B0890). This product is intended for research and analytical applications. Zomepirac sodium salt (McN-2783-21-98) is an orally active prostaglandin synthetase inhibitor. Zomepirac sodium salt blocks prostaglandin synthesis and inhibits Collagen (HY-P72147)- or Epinephrine (HY-B0447)-induced platelet aggregation. Zomepirac sodium salt can be used for the research of postoperative pain and osteoarthritis.

AF3485 is a human mPGES-1 inhibitor that exhibits antitumor activity in vitro and in vivo. AF3485 inhibits tumor-associated angiogenesis by reducing PGE2 production, inhibiting EGFR signaling, and decreasing VEGF and FGF-2 expression. AF3485 reduced tumor growth in mice bearing human A431 xenograft tumors by subchronic administration.