VU0483605

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VU0483605

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Cat No: 16941

Biochemicals - Receptor Pharmacology

Glutamate, the major excitatory neurotransmitter in the CNS, activates eight known subtypes of metabotropic glutamate receptors (mGluRs). Highly selective modulators designed to act at allosteric sites on certain mGluR subtypes are being developed to p...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

3-chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-2-pyridinecarboxamide

Correlated keywords:

Glutamate neuroscience metabotropic glutamate receptor mGluR1 positive allosteric modulator PAM schizophrenia biochemical signal transduction biochemistry intracellular signaling VU-0483605 selective mGlu1 reduction mediated calcium mutant cells CNS central nervous system

Product Overview:
Glutamate, the major excitatory neurotransmitter in the CNS, activates eight known subtypes of metabotropic glutamate receptors (mGluRs). Highly selective modulators designed to act at allosteric sites on certain mGluR subtypes are being developed to preferentially regulate subtype-specific, glutamate-induced receptor activation.{22053} VU0483605 is a selective positive allosteric modulator (PAM) of mGluR1, displaying EC50 values of 0.39 and 0.36 μM at human and rat receptors, respectively, and no activity as a mGlu4 PAM (EC50 >10 μM).{27299} It has been shown to potentiate a response to glutamate in wild-type cell lines stably expressing mGlu1 and to partially restore the reduction in glutamate-mediated calcium signaling in a mutant cell model of schizophrenia.{27299}

Size	1 mg
Shipping	dry ice
CAS Number	1623101-11-0
Molecular Formula	C₂₀H₁₀Cl₃N₃O₃
SMILES	O=C1N(C2=CC=C(NC(C3=C(Cl)C=CC=N3)=O)C=C2Cl)C(C4=CC=CC(Cl)=C41)=O
Molecular Weight	446,7
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
UNSPSC code	12352100

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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.

Accreditations
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.