668463-35-2
668463-35-2
Chemical Structure
RPR-260243
- CAS No.: 668463-35-2
- Formula:C28H25F3N2O4
- Molecular Weight:510.50
IUPAC 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
InChIKey: VWNMWKSURFWKAL-HXOBKFHXSA-N
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
Biological Activity: 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.
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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RPR-260243 | 98.01% | 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. | ||||||||||||||||||||
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Viquidil | Viquidil (Quinotoxine), an isomer of Quinidine, is a cerebral vasodilator agent. Viquidil shows antithrombotic activity. | |||||||||||||||||||||
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Viquidil hydrochloride | 99.93% | Viquidil hydrochloride (Quinotoxine hydrochloride), an isomer of Quinidine, is a cerebral vasodilator agent. Viquidil hydrochloride shows antithrombotic activity. | ||||||||||||||||||||
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Viquidacin | Viquidacin (NXL 101) is an antibiotic with inhibitory activity against topoisomerase IV and DNA gyrase. Viquidacin exhibits antibacterial activity against gram positive bacterial by inhibiting the supercoiling, decatenation and relaxation in strains Staphylococcus aureus and Escherichia coli in micromolar levels. Viquidacin inhibits S. aureus wildtype and mutants with MIC of 2-128 mg/L. | |||||||||||||||||||||
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Hydroquinine | 99.87% | Hydroquinine (Dihydroquinine) is an anti-bacterial agent that inhibits both Gram-positive and Gram-negative bacteria. Hydroquinine inhibits the growth of multidrug-resistant pseudomonas aeruginosa via the suppression of the arginine deiminase pathway genes. Hydroquinine inhibits Plasmodium falciparum and Plasmodium berghei. Hydroquinine displays anti-malarial and demelanizing activities. Hydroquinine effectively induces specific RND-type efflux pump systems in Pseudomonas aeruginosa, particularly the MexCD-OprJ and MexXY efflux pumps. Hydroquinine inhibits Pseudomonas aeruginosa adhesion and biofilm formation. Hydroquinine serves as a precursor for derivatives such as C9 epihydroquinine, 9-acetoxy-10,11-dihydroquinine, and 10,11-dihydroquinine monohydrochloride. | ||||||||||||||||||||
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Quinine hydrochloride dihydrate (Standard) | ≥98% | Quinine (hydrochloride dihydrate) (Standard) is the analytical standard of Quinine (hydrochloride dihydrate). This product is intended for research and analytical applications. Quinine hydrochloride dihydrate (Qualaquin) is an orally active and can be used in anti-malarial studies. Quinine hydrochloride dihydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC50 of 169 μM. | ||||||||||||||||||||
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Hydroquinidine (Standard) | ≥98% | Hydroquinidine (Standard) is the analytical standard of Hydroquinidine. This product is intended for research and analytical applications. Hydroquinidine (Dihydroquinidine) is a derivative of Quinidine (an antiarrhythmic agent). Hydroquinidine prolongs the QT interval and has antiarrhythmic efficacy. | ||||||||||||||||||||
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Quinine sulfate | 99.38% | Quinidine sulfate is an antiarrhythmic agent. Quinidine sulfate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine sulfate is also a K+ channel blocker with an IC50 of 19.9 μM. Quinidine sulfate can be used for malaria research. | ||||||||||||||||||||
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Quinidine gluconic acid | Quinidine gluconic acid is an orally active antiarrhythmic agent. Quinidine gluconic acid reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine gluconic acid exerts sustained block and open-channel block effects on IK(f). Quinidine gluconic acid alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine gluconic acid can be used in studies related to uterine sarcoma and seizures. | |||||||||||||||||||||
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Hydroquinidine hydrochloride | Hydroquinidine hydrochloride is a potent ion channel blocker, which exhibits strong anti-cancer activity on colon, pancreatic, and hepatocellular cancer cells. Hydroquinidine hydrochloride prolongs the QT interval and has antiarrhythmic efficacy. | |||||||||||||||||||||
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Quininone | Quininone is a Quinine (HY-D0143) derivative that exhibits in vitro antifungal activity. Quininone can be used for antifungal research. | |||||||||||||||||||||
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References
- [1]. Wu W, et al. Concatenated hERG1 tetramers reveal stoichiometry of altered channel gating by RPR-260243. Mol Pharmacol. 2015;87(3):401-409. [Content Brief]
- [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. [Content Brief]
