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RPR-260243

CAT: 0804-HY-16915-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-16915-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC50=58 nM) . RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel[1][2]. RPR-260243 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
CAS Number
668463-35-2
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Potassium Channel
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel
Applications
COVID-19-immunoregulation
Field of Research
Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/RPR-260243.html
Purity
99.91
Solubility
DMSO : 10 mg/mL (ultrasonic)
Smiles
O=C([C@H]1CN(CC#CC2=CC(F)=CC(F)=C2F)CC[C@H]1CCC(C3=CC=NC4=CC=C(OC)C=C34)=O)O
Molecular Formula
C28H25F3N2O4
Molecular Weight
510.50
Precautions
H302, H315, H319, H335
References & Citations
[1]Wu W, et al. Concatenated hERG1 tetramers reveal stoichiometry of altered channel gating by RPR-260243. Mol Pharmacol. 2015;87 (3) :401-409.|[2]Kang J, et al. Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Mol Pharmacol. 2005;67 (3) :827-836.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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