Nepicastat (hydrochloride)

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Cat No: 22126

Biochemicals - Small Molecule Inhibitors

Nepicastat is an inhibitor of dopamine β-hydroxylase (DBH; IC50 = 9 nM for the purified human enzyme).{45348} It is selective for DBH over a panel of 12 enzymes and 13 neurotransmitter receptors (IC50s or Kis = >10 μM). Nepicastat dose-dependently red...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

5-(aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione, monohydrochloride

Correlated keywords:

173997-05-2 hydrolase DBH neuro-transmitter RS-25560197 RS25560197 RS25560-197

Product Overview:
Nepicastat is an inhibitor of dopamine β-hydroxylase (DBH; IC50 = 9 nM for the purified human enzyme).{45348} It is selective for DBH over a panel of 12 enzymes and 13 neurotransmitter receptors (IC50s or Kis = >10 μM). Nepicastat dose-dependently reduces norepinephrine content and increases dopamine content in the mesenteric artery, left ventricle, and cerebral cortex in spontaneously hypertensive rats, as well as in the renal artery, left ventricle, and cerebral cortex in beagle dogs. It attenuates increases in diastolic blood pressure and heart rate induced by preganglionic sympathetic nerve stimulation in pithed spontaneously hypertensive rats when administered orally at doses of 10 and 30 mg/kg.{45349} Nepicatstat (50 mg/kg) reduces the progressive ratio response for cocaine, but not food or sucrose pellets, in rats.{45350} It also reduces reinstatement of cocaine-seeking behavior induced by cues, yohimbine (Item No. 19869), or foot-shock in rats.

Size	1 mg
Shipping	dry ice
CAS Number	170151-24-3
Molecular Formula	C₁₄H₁₅F₂N₃S • HCl
SMILES	FC1=CC(F)=C(CC[C@H](N2C(CN)=CNC2=S)C3)C3=C1.Cl
Molecular Weight	331,8
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
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.

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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.