CAY10678

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CAY10678

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Cat No: 15129

Biochemicals - Small Molecule Inhibitors

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2.{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.{11537} C...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-cyclopentyl-1-[5,6-dimethyl-1-(1-methylethyl)-1H-benzimidazol-2-yl]-4-piperidinecarboxamide

Correlated keywords:

inhibitors cyclooxygenases inflammation pains COXs inhibits inhibitions prostaglandins PGs PGES mPGES CAYs 10678 CAY-10678 benzoimidazole synthesis microsomal synthase hematopoietic lipocalin potent mPGES1 mPGES-1 1 one E synthase-1 PGH2 PGH 2 two PGE2 COX-2 induced pro-inflammatory proinflammatory pro inflammatory mediators LPS IL-1.beta. IL-1beta IL-1B IL-1? ? IL beta .beta. interleukins TNF-? TNF-alpha TNF-.alpha. alpha .alpha. ? TNFs humans rats recombinant COX-1 PGIS PGDS lipocalin-type dose-dependent doses dependents blocks cells blood recruitment mice

Product Overview:
Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2.{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.{11537} CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively).{23940} It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 μM but reduces lipocalin-type PGDS activity by 60% at this concentration.{23940} CAY10678 dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β.{23940} It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice.{23940}

Size	1 mg
Shipping	dry ice
CAS Number	1268709-57-4
Molecular Formula	C₂₃H₃₄N₄O
SMILES	O=C(C1CCN(C2=NC3=CC(C)=C(C)C=C3N2C(C)C)CC1)NC4CCCC4
Molecular Weight	382,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.39
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.