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373501 Herg Activator, NS1643 - CAS 448895-37-2 - Calbiochem

373501
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₅H₁₀F₆N₂O₃

Products

Catalogue NumberPackaging Qty/Pack
373501-10MG Glass bottle 10 mg
Description
OverviewA diphenolurea compound that selectively activates human ether-a-go-go-related gene (hERG) K+-channel (EC50 = 10.5 µM). Shown to significantly increase both steady-state and peak tail currents of hERG channels, but exhibits only a trivial effect on Kv4.3 and Kv1.5 channels. Causes a significant reduction in action potential duration (APD90 ) in patch clamp assays in Xenopus oocytes, HEK293 cells, and guinea pig cardiamyocyes that can be reversed by the addition of E-4031 (Cat. No. 324470), a specific blocker of hERG channels. Also shown to activate IKr channel in cardiomyocytes and increase post-repolarization refractory time thereby alleviating hyper-excitability and producing antiarrhythmic effects. It can also restore IKr reduced by down-regulation of IKr expression.
Catalogue Number373501
Brand Family Calbiochem®
SynonymsHuman ether-a-go-go related gene (hERG) K+ channel activator, 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea, NS 1643, KV11.1 Channel Activator
References
ReferencesHansen, R., et al. 2006. Mol. Pharm. 69, 266.
Schuster, A., et al. 2011. Mol. Pharm. 80, 930.
Product Information
CAS number448895-37-2
FormOff-white powder
Hill FormulaC₁₅H₁₀F₆N₂O₃
Chemical formulaC₁₅H₁₀F₆N₂O₃
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freee (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

Herg Activator, NS1643 - CAS 448895-37-2 - Calbiochem Certificates of Analysis

TitleLot Number
373501

References

Reference overview
Hansen, R., et al. 2006. Mol. Pharm. 69, 266.
Schuster, A., et al. 2011. Mol. Pharm. 80, 930.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision13-July-2012 JSW
SynonymsHuman ether-a-go-go related gene (hERG) K+ channel activator, 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea, NS 1643, KV11.1 Channel Activator
DescriptionA diphenolurea compound that selectively activates human ether-a-go-go-related gene (hERG) K+-channel (EC50 = 10.5 µM). Shown to significantly increase both steady-state and peak tail currents of hERG channels, but exhibits only a trivial effect on Kv4.3 and Kv1.5 channels. Causes a significant reduction in action potential duration (APD90 ) in patch clamp assays in Xenopus oocytes, HEK293 cells, and guinea pig cardiamyocyes that can be reversed by the addition of E-4031 (Cat. No. 324470), a specific blocker of hERG channels. Also shown to activate IKr channel in cardiomyocytes and increase post-repolarization refractory time thereby alleviating hyper-excitability and producing antiarrhythmic effects. It can also restore IKr reduced by down-regulation of IKr expression.
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number448895-37-2
Chemical formulaC₁₅H₁₀F₆N₂O₃
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml; clear, nearly colorless solution)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freee (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesHansen, R., et al. 2006. Mol. Pharm. 69, 266.
Schuster, A., et al. 2011. Mol. Pharm. 80, 930.