SR 17018

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SR 17018

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Cat No: 24480

Biochemicals - Receptor Pharmacology

SR 17018 is an orally bioavailable and brain-penetrant agonist of μ-opioid receptors.{40627} It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTPγS binding in CHO cells expressing μ-opioid receptors) over β-arres...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

5,6-dichloro-1-[1-[(4-chlorophenyl)methyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one

Correlated keywords:

SR17018 GPCR S 186.006 S186.006

Product Overview:
SR 17018 is an orally bioavailable and brain-penetrant agonist of μ-opioid receptors.{40627} It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTPγS binding in CHO cells expressing μ-opioid receptors) over β-arrestin 2 recruitment (EC50 = >10,000 nM) at the μ-opioid receptor. SR 17018 increases latency to withdraw in the hot plate and warm water tail-flick assay (ED50s = 6.9 and 7.7 mg/kg, respectively) without inducing respiratory depression in mice when administered at doses up to 48 mg/kg. SR 17018 was designed for this biased agonism at the μ-opioid receptor to potentially widen the therapeutic window and reduce adverse effects of μ-opioid receptors, such as respiratory depression.

Size	1 mg
Shipping	dry ice
CAS Number	2134602-45-0
Molecular Formula	C₁₉H₁₈Cl₃N₃O
SMILES	ClC(C=C1)=CC=C1CN2CCC(N3C(NC4=C3C=C(Cl)C(Cl)=C4)=O)CC2
Molecular Weight	410,7
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.39
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.