Name: Co 102862
Brand: Alomone Labs
SKU: C-160

Overview

Cat #: C-160

Alternative Name V102862

Lyophilized Powder yes

Source Synthetic

MW: 273.3

Purity: >96% (HPLC)

Effective concentration 0.1-200 μM

Structure

Chemical name 2-[[4-(4-Fluorophenoxy)phenyl]methylene]hydrazinecarboxamide.

Molecular formula C₁₄H₁₂FN₃O₂.

CAS No.: 181144-66-1

Activity Co 102862 is a potent, broad spectrum and state-dependent blocker of neuronal voltage-gated Na⁺ channels that interacts selectively with inactivated states as opposed to resting states of the channel¹. IC₅₀ values are 0.28-15.9 µM in rat hippocampal neurons². It is an anticonvulsant, demonstrating potent activity in rodent models of tonic/clonic and partial-complex seizures³.

References-Activity

Catterall, W.A. (1992) Physiol. Rev. 72, S15.
Ilyin, V.I. et al. (2005) Br. J. Pharmacol. 144, 801.
Carter, R.B. et al. (1997) Soc. Neurosci. Absrt. 23, 2163.

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.

Solubility DMSO. 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.

Our bioassay

Alomone Labs Co 102862 inhibits Na_V1.7 channel currents in HEK293 cells.
A. Time course of current reversible inhibition by 50 µM Co 102862 (#C-160). 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 application of 50 µM Co 102862.

References - Scientific background

Catterall, W.A. (1992) Physiol. Rev. 72, S15.
Catterall, W.A. (2000) Neuron 26, 13.
Bean, B.P. et al. (1983) J. Gen. Physiol. 81, 613.
Hondeghem, L.M. and Katzung, B.G. (1984) Annu. Rev. Pharmacol. Toxicol. 24, 387.
Butterworth, J.F. 4th and Strichartz, G.R. (1990) Anesthesiology 72, 711.
Kuo, C.C. and Bean, B.P. (1994) Mol. Pharmacol. 46, 716.
Xie, X.M. et al. (1995) Pfluegers Arch. Eur. J. Physiol. 430, 437.
Kuo, C.C. et al. (1997) Mol. Pharmacol. 51, 1077.
Kuo, C.C. et al. (2000) Mol. Pharmacol. 57, 135.
Yang, Y.C. and Kuo, C.C. (2002) Mol. Pharmacol. 62, 1228.
Ilyin, V.I. et al. (2005) Br. J. Pharmacol. 144, 801.
Carter, R.B. et al. (1997) Soc. Neurosci. Absrt. 23, 2163.

Scientific background

Voltage-gated Na⁺ channels play key roles in determining neuronal excitability^1,2. Voltage- and use-dependent blockage of voltage-gated Na⁺ channels appear to be important in the mechanism of action of many anticonvulsants (e.g. phenytoin (PHT), carbamazepine (CBZ) and lamotrigine (LTG)), local anesthetics (e.g. lidocaine and bupivacaine) and Class I antiarrhythmics^3-10.

Co 102862 is a potent, broad spectrum and state-dependent blocker of neuronal voltage-gated Na⁺ channels that interacts selectively with inactivated states as opposed to resting states of the channel¹¹. IC₅₀ values are 0.28-15.9 μM in rat hippocampal neurons¹¹.

Co 102862 is an anticonvulsant, demonstrating potent activity in rodent models of tonic/clonic and partial-complex seizures¹².

Target Na_V Na⁺ channels

Lyophilized Powder

Co 102862 (#C-160) is a highly pure, synthetic, and biologically active compound.

Certificate of Analysis SDS

For research purposes only, not for human use

Last Update: 07/05/2024

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Co 102862

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