SR 48692

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SR 48692

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Cat No: 20124

Biochemicals - Receptor Pharmacology

SR 48692 is an orally bioavailable allosteric antagonist of the neurotensin receptor NTS1 (Kd = 3.4 nM).{35296,35297} SR 48692 inhibits high affinity neurotensin binding to brain tissue from guinea pig, newborn mouse, newborn human, and adult human as...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid

Correlated keywords:

Meclinertant SR48692 NTS-1 HT29 NCIH209 NCIH345

Product Overview:
SR 48692 is an orally bioavailable allosteric antagonist of the neurotensin receptor NTS1 (Kd = 3.4 nM).{35296,35297} SR 48692 inhibits high affinity neurotensin binding to brain tissue from guinea pig, newborn mouse, newborn human, and adult human as well as rat mesencephalic cells and HT-29 cells with IC50 values ranging from 0.99 to 30.3 nM.{35296} It blocks neurotensin-induced intracellular calcium mobilization in HT-29 cells with a Ki value of 7.4 nM. SR 48692 (10 μM) inhibits NCI-H209 and NCI-H345 cell proliferation by approximately 70 and 80%, respectively.{35299} In vivo, SR 48692 (10 μg per day) reduces tumor volume and cell proliferation in an NCI-H209 mouse xenograft model. SR 48692 (80 μg/kg, p.o.) reduces contralateral turning induced by neurotensin (Item No. 24717) administration in mice by 85%.{35296} Daily administration of SR 48692 for five days in rats delays sensitization to the locomotor activating effects of cocaine during three additional cocaine challenges when given seven days prior to cocaine delivery but not under a cotreatment regimen.{35298}

Size	1 mg
Shipping	dry ice
CAS Number	146362-70-1
Molecular Formula	C₃₂H₃₁ClN₄O₅
SMILES	COC1=CC=CC(OC)=C1C2=CC(C(N[C@@]3(C(O)=O)[C@@H](C4)C[C@@H]5C[C@H]3C[C@H]4C5)=O)=NN2C6=C(C=CC(Cl)=C7)C7=NC=C6
Molecular Weight	587,1
Formulation	A solid
Purity	≥98%
Custom Code	2922.19
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.