MK-0524

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MK-0524

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Cat No: 10009835

Biochemicals - Receptor Pharmacology

MK-0524 is a potent, selective prostaglandin D2 (PGD2)receptor DP1 antagonist with Ki values of 0.57 nM and 0.75 µM for the DP1 and DP2 receptors, respectively.{14713} It inhibits PGD2-induced accumulation of cAMP in both washed platelets and platelet...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(3R)-4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-cyclopent[b]indole-3-acetic acid

Correlated keywords:

MK0524 PGD2 DP2 DP1 ALS DP-1 PGD-2 amyotrophic lateral sclerosis

Product Overview:
MK-0524 is a potent, selective prostaglandin D2 (PGD2)receptor DP1 antagonist with Ki values of 0.57 nM and 0.75 µM for the DP1 and DP2 receptors, respectively.{14713} It inhibits PGD2-induced accumulation of cAMP in both washed platelets and platelet-rich plasma with IC50 values of 0.09 and 4.0 nM, respectively.{14713} In a sheep model of allergic rhinitis, 0.1 mg/kg MK-0524 completely blocked PGD2-induced nasal congestion.{14713} At a dose of 4 mg/kg, MK-0524 suppressed a nicotinic acid-induced vasodilatory response by 80% in a mouse model of flushing, an undesirable side-effect of niacin treatment for dyslipidemia.{15245} In an in vitro model of amyotrophic lateral sclerosis, MK-0524 has been shown to partially protect cultured motor neurons from PGD2-induced toxicity.{33495,33496}

Size	1 mg
Shipping	dry ice
CAS Number	571170-77-9
Molecular Formula	C₂₁H₁₉ClFNO₄S
SMILES	FC1=CC2=C(N(CC3=CC=C(Cl)C=C3)C4=C2CC[C@@H]4CC(O)=O)C(S(C)(=O)=O)=C1
Molecular Weight	435,9
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2930.90
UNSPSC code	12352100

Cheng, K., Wu, T., Wu, K.K., et al. Antagonism of the prostaglandin D₂ receptor 1 suppresses nicotinic acid-induced vasodilation in mice and humans. Proc Natl Acad Sci USA 103(17) 6682-6687 (2006).

Sturino, C.F., O'Neill, G., Lachance, N.

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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.