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VU0360223

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    VU0360223
  • VU0360223
Cat No: 11995
Biochemicals - Receptor Pharmacology
Cayman

Glutamate, the major excitatory neurotransmitter in the central nervous system, signals through both ionotropic and metabotropic glutamate receptors. Of the eight metabotropic glutamate receptors (mGlus) discovered thus far, development of inhibitors t...

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Territorial Availability: Available through Bertin Technologies only in France
Synonyms:
  • 3-fluoro-5-(2-methyl-5-benzothiazolyl)-benzonitrile
Correlated keywords:
  • receptors negative allosteric modulators neuroscience glutamate mGlu receptors VU-0360223 VU0360223 mGluR5 mGlu1-4 mGlu7-8 plasma brain in vivo CAY10651 CAY 10651 10820
Product Overview:
Glutamate, the major excitatory neurotransmitter in the central nervous system, signals through both ionotropic and metabotropic glutamate receptors. Of the eight metabotropic glutamate receptors (mGlus) discovered thus far, development of inhibitors to mGlu5 has been given significant attention in preclinical models of disease, including pain, anxiety, gastresophageal reflux disease, Parkinson’s associated dyskinesia, and fragile X syndrome, as well as in animal models of drug addiction. VU0360223 is a noncompetitive antagonist (negative allosteric modulator) of mGlu5 that demonstrates an IC50 value of 61 nM in a calcium mobilization assay and a Ki value of 477 nM in a radioligand binding assay.{19263} A 10 μM concentration of VU0360223 results in a near complete blockade of the glutamate response in cortical astrocytes.{19263} A 30 mg/kg dose of VU0360223 in mice yields potent inhibition in a marble burying model of anxiety and is efficacious in an operant sensation seeking model of addiction.{19263}
Size 1 mg
Shipping dry ice
CAS Number 1274859-33-4
Molecular Formula C15H9FN2S
SMILES FC1=CC(C#N)=CC(C2=CC3=C(SC(C)=N3)C=C2)=C1
Molecular Weight 268,3
Formulation A crystalline solid
Purity ≥98%
Custom Code 2903.99
UNSPSC code 12352100

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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.

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