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.
Product information
CAS Number: 668463-35-2
Molecular Weight: 510.50
Formula: C28H25F3N2O4
Chemical Name: (3R,4R)-4-[3-(6-methoxyquinolin-4-yl)-3-oxopropyl]-1-[3-(2,3,5-trifluorophenyl)prop-2-yn-1-yl]piperidine-3-carboxylic acid
Smiles: COC1C=C2C(=CC=NC2=CC=1)C(=O)CC[C@@H]1CCN(C[C@@H]1C(O)=O)CC#CC1=CC(F)=CC(F)=C1F
InChiKey: VWNMWKSURFWKAL-HXOBKFHXSA-N
InChi: InChI=1S/C28H25F3N2O4/c1-37-20-5-6-25-22(15-20)21(8-10-32-25)26(34)7-4-17-9-12-33(16-23(17)28(35)36)11-2-3-18-13-19(29)14-24(30)27(18)31/h5-6,8,10,13-15,17,23H,4,7,9,11-12,16H2,1H3,(H,35,36)/t17-,23+/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 10 mg/mL (19.59 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
RPR-260243 enhances the delayed rectifier current in guinea pig myocytes but, when administered alone, has little effect on action potential parameters in these cells.
Products are for research use only. Not for human use.
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