product summary
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company name :
Alomone Labs
product type :
chemical
product name :
Pilsicainide hydrochloride
catalog :
P-145
more info or order :
image
image 1 :
Alomone Labs P-145 image 1
Alomone LabsIndisetron dihydrochlorideblocks 5-HT3A channels expressed in HEK 293T cells. - 5-HT3A channel currents were elicited by 10 M 5-HT delivered every 3 minutes.Indisetron dihydrochloride(#I-175) was applied 30 seconds before stimulation at 100 nM as indicated and inhibited the 5-HT induced current in a dose dependent and reversible manner.
image 2 :
Alomone Labs P-145 image 2
Alomone Labs Pilsicainide hydrochloride inhibits NaV1.7 channels expressed in HEK293 cells. - A. Time course of current reversible inhibition by 100 ?MPilsicainide hydrochloride(#P-145). Currents were elicited by a voltage ramp from a holding potential of -100 mV to 60 mV (30 ms) delivered every 10 seconds. B. Example traces of current response to voltage ramp stimulation before and during 100 ?M Pilsicainide hydrochloride application.
product information
CAT :
P-145
SKU :
P-145_10 mg
Product Name :
Pilsicainide hydrochloride
Group Type :
Non Antibodies
Product Type :
S. Molecules
Storage After Reconstitution :
The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.
Shipping and storage :
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Product Page - Scientific background :
Voltage-gated Na+ channels (VGSC, NaV) are critically important for electrogenesis and nerve impulse conduction. Certain Na+ channel isoforms are predominantly expressed in peripheral sensory neurons associated with pain sensation, and the expression and functional properties of Nav in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation1.Pilsicainide is a class IC anti-arrhythmic drug widely used in the treatment of supraventricular and ventricular tachyarrhythmias in Japan2. Results from voltage clamp experiments show that Pilsicainide is a pure Na+ channel blocker with little or no effect on other cardiac channels, probably with the exception of HERG channels3-5.Measurements of Pilsicainide's ability to block hNaV1.4 channels resulted in half-maximum inhibitory concentrations (IC50) of 189 ± 10 µM at 0.1 Hz, and 76 ± 7 µM at 10 Hz. Effects of Pilsicainide were similar on skeletal muscle hNaV1.4, brain hNaV1.1 and heart hNaV1.5 channels.
Supplier :
Alomone Labs
Target :
TTX-Sensitive NaV channels
Long Description :
Pilsicainide hydrochloride (#P-145) is a highly pure, synthetic, and biologically active compound.
Short Description :
A Use-Dependent Anti-Arrhythmic NaV Channel Blocker
MW :
308.85
Synonyms :
SUN 1165
Source :
Synthetic
Molecular formula :
C17H24N2O•HCl.
Effective Concentration :
10-200 µM.
Activity :
Pilsicainide hydrochloride is an anti-arrhythmic drug1 and activity dependent Na+ (NaV) channel blocker2. Pilsicainide hydrochloride blocks human NaV1.4 channels with IC50s of 189 ± 10 µM at 0.1 Hz and 76 ± 7 µM at 10 Hz3.
Reconstitution and Solubility :
Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity.
Solubility :
Water. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions :
Up to four weeks at 4°C or three months at -20°C.
Lead Time :
1-2 Business Days
Country of origin :
Israel/IL
Applications key :
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Purity :
>99%
CAS No :
88069-49-2
Form :
Lyophilized powder.
Comment :
Contact Alomone Labs for technical support and product customization
UNSPSC :
41116134
Bioassay Tested :
Yes
Chemical Name :
N-(2,6-Dimethylphenyl)tetrahydro-1H-pyrrolizine-7a(5H)-acetamide hydrochloride.
more info or order :
company information
Alomone Labs
Jerusalem BioPark (JBP), Hadassah Ein Kerem
P.O. Box 4287
Jerusalem 9104201
info@alomone.com
http://www.alomone.com
972 2 531 8002
headquarters: Israel