GS-39783

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GS-39783

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Cat No: 29482

Biochemicals - Receptor Pharmacology

GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).{53122} It amplifies GABAB recept...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N4,N6-dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine

Correlated keywords:

GS39783 GABA-B GTP?-S GTP-?S HEK-293 MK801 anti-psychotic

Product Overview:
GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).{53122} It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM). GS-39783 (25-100 mg/kg) suppresses alcohol self-administration, but has no effect on lever-responding for food, in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats.{53123} It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity.{53124} GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).{53125}

Size	5 mg
Shipping	dry ice
CAS Number	39069-52-8
Molecular Formula	C₁₅H₂₃N₅O₂S
SMILES	CSC1=NC(NC2CCCC2)=C([N+]([O-])=O)C(NC3CCCC3)=N1
Molecular Weight	337,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.59
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.