RPR-260243

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. 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.


Cat. No.: EX-A13153	Purity: >98%

	Chemical structure of RPR-260243

For research only, Do not use for Human!

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CAS No.	668463-35-2
Purity	>98%
Formula	C28H25F3N2O4
Mol Weight	510.5043
Color	Light yellow to light brown
State	Solid
Solubility	DMSO : 10 mg/mL
Shelf Life	>3 years if stored properly
Storage	Powder -20°C, 3 years , 4°C, 2 years; In solvent -20°C, 1 month
Shipping	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Reference:	[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.
CoA	CoA of RPR-260243

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


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