GAT211

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GAT211

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Cat No: 24484

Biochemicals - Receptor Pharmacology

GAT211 is an agonist and positive allosteric modulator (PAM) of cannabinoid receptor 1 (CB1) and a racemic mixture of GAT228 (Item No. 24485) and GAT229 (Item No. 24486), which have enantiomer-specific activities.{35179} GAT211 increases β-arrestin re...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

3-(2-nitro-1-phenylethyl)-2-phenyl-1H-indole

Correlated keywords:

1428527-93-8 GAT 211 CB1 CB 1 GAT 228 229 HEK 293A hCB1GFP hCB CP55940 2AG 55940 ERK12 PLC ?3 EPSC

Product Overview:
GAT211 is an agonist and positive allosteric modulator (PAM) of cannabinoid receptor 1 (CB1) and a racemic mixture of GAT228 (Item No. 24485) and GAT229 (Item No. 24486), which have enantiomer-specific activities.{35179} GAT211 increases β-arrestin recruitment and cAMP inhibition in HEK293A cells expressing GFP-tagged human CB1 (hCB1-GFP) in a concentration-dependent manner. It also enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing hCB1, as well as the activity of 2-arachidonoyl glycerol (2-AG; Item No. 62160), arachidonoyl ethanolamide (AEA; Item No. 90050), and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. It inhibits excitatory postsynaptic currents (EPSCs) in a subset of CB1-expressing murine autaptic hippocampal neurons when used at a concentration of 1 µM.{48089} GAT211 also decreases mechanical hypersensitivity in wild-type (EC50 = 9.75 mg/kg), but not CB1 knockout, mice in a model of inflammatory pain induced by complete Freund’s adjuvant (CFA), and decreases mechanical and cold allodynia in a mouse model of paclitaxel-induced neuropathic pain when used at doses of 10 and 20 mg/kg per day.{47206}

Size	1 mg
Shipping	dry ice
CAS Number	102704-40-5
Molecular Formula	C₂₂H₁₈N₂O₂
SMILES	O=[N+](CC(C1=CC=CC=C1)C2=C(C3=CC=CC=C3)NC4=CC=CC=C42)[O-]
Molecular Weight	342,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2921.49
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.