-
-
Overview
-
Please contact us at for specific academic pricing.
Background
Description:
IC50 Value: 0.11uM (for N-type Calcium channel) [1]
NP-118809 is a potent N-type calcium channel blockers which have good selectivity over L-type calcium channels.
in vitro: NP-118809, exhibited increased N-type channel blockade (IC50=0.11 uM) and was 111-fold more selective for N-type channels (L-type calcium channel IC50=12.2 uM) [1]. In the N,4-dibenzhydryl-piperazine-1-carboxamide series (21-27), non-substituted derivative (21) showed a similar inhibitory activity for N-type calcium channels (est. IC50=0.15 uM) as that of parent compound, NP-118809 (est. IC50=0.11 uM). 1-[Phenyl(pyridin-4-yl)methyl]piperazine (42), with no substituent on the nitrogen showed good N-type blocking activity (est. IC50=0.06 uM) while the N-methylated analog (43) was an order of magnitude less potent (est. IC50=0.69 uM) [2].
in vivo: NP-118809, i.v. at 2 mg/kg or p.o. at 10 mg/kg in rats, showed acceptable absorption (Tmax=2.3 hr) and half-life (2.1 hr) characteristics and a mean oral bioavailability of 30%. Both compounds were widely distributed outside of plasma and/or bound to plasma proteins. Upon i.p. administration of NP-118809 and NP-078585 at 25 mg/kg, both showed analgesic activity in Phase IIA portions of the rat formalin model. A single 1 uM dose application of NP-078585 blocked hERG currents showing its potential for cardiovascular liability [1].
Clinical trial:
-
- Properties
-
Overview
- Home
- Products
- Life Science
- Analytical Chromatography
- Assay Kits
- Biochemical Reagents
- Antibodies
- Antigens
- Enzymes
- Chemicals
- Proteins
- Liposomes
- Cell Culture
- Cell Analysis
- Cloning and Expression
- Nucleic Acid Synthesis
- Nucleic Acid Extraction
- Nucleic Acid Electrophoresis
- PCR
- Protein Gel Electrophoresis
- Protein Biochemistry
- Nanoparticles
- Glycan Analysis
- Immunohistochemistry (IHC)
- Microbiology
- Biospecimens
- Transfection Reagents
- Ion Exchange Resins
- Venoms
- Lab Solutions
- Lab Equipment
- Biosensors
- Flow Imaging Microscopes
- Fluorescence Quality Management Solutions
- Electrophoresis Systems
- Hematology Analyzers
- Isothermal Amplification Instruments
- Liquid Handling Equipment
- Luminometers
- Microfluidic Flow Control Systems
- Next-generation Sequencing Systems
- Nucleic Acid Purification Instruments
- Raman Spectroscopy Systems
- Sample Tracking Systems
- Spectrometer Accessories
- Syringe Pumps
- Thawing and Warming Systems
- Tissue Dissociation Systems
- Water Purification Systems
- Western Blotting Equipment
- General Laboratory Equipment
- Clinical Chemistry Analyzers
- Amerigo Scientific Instrument
- Automated Cell Selection Systems
- Automated Nucleic Acid Extraction Instruments
- Balances, Scales and Weighing
- Biolayer Interferometry Instruments
- Bioprocess Filtration Equipment
- Bioprocess Systems and Accessories
- Bioreactors and Fermenters
- Cappers and Decappers
- Cell Thawing Instruments
- Chromatography
- Data Loggers
- Droplet Generators
- Dry Baths
- Flow Cytometers
- Histology Laboratory Equipment
- Lab Ovens and Furnaces
- Lab Refrigeration Equipment
- Lab Shakers and Mixers
- Laboratory Centrifuges
- Laboratory Evaporators
- Laboratory Hoods
- Laboratory Incubators
- Laboratory Microscopes
- Laboratory Mills
- Laboratory Pumps
- Liquid Handling
- Live Cell Imaging Systems
- Microbiology Equipment
- Microscopy Flow Cells
- Mutation Breeding Instruments
- Oligonucleotide Synthesis Devices
- Particle Counters
- Plasma Surface Treatment Equipment
- Presses and Pellet Dies
- Surface Plasmon Resonance Instruments
- Ultrasonic Cleaners
- UV Disinfection Systems
- VOC Analysis Equipment
- VPHP Sterilization Systems
- Water Baths
- Lab Equipment
- Diagnostics & Clinical
- Applied Science
- Life Science
- Services
- About Us
- Contact Us
.
