WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H532579
CAS#: 668463-35-2
Description: RPR260243 is a novel activator of HERG. It modifies HERG currents inhibited by dofetilide (IC50 = 58 nM). RPR260243 has little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.
Hodoodo Cat#: H532579
Name: RPR260243
CAS#: 668463-35-2
Chemical Formula: C28H25F3N2O4
Exact Mass: 510.18
Molecular Weight: 510.510
Elemental Analysis: C, 65.88; H, 4.94; F, 11.16; N, 5.49; O, 12.54
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Synonym: RPR260243; RPR 260243; RPR-260243.
IUPAC/Chemical Name: (3R,4R)-4-[3-(6-methoxyquinolin-4-yl)-3-oxopropyl]-1-[3-(2,3,5-trifluorophenyl)prop-2-ynyl]piperidine-3-carboxylic acid
InChi Key: VWNMWKSURFWKAL-HXOBKFHXSA-N
InChi Code: 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
SMILES Code: 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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: 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.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 510.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Gardner A, Sanguinetti MC. C-Linker Accounts for Differential Sensitivity of ERG1 and ERG2 K+ Channels to RPR260243-Induced Slow Deactivation. Mol Pharmacol. 2015 Jul;88(1):19-28. doi: 10.1124/mol.115.098384. Epub 2015 Apr 17. PubMed PMID: 25888115; PubMed Central PMCID: PMC4468633.
2: Wu W, Gardner A, Sanguinetti MC. Concatenated hERG1 tetramers reveal stoichiometry of altered channel gating by RPR-260243. Mol Pharmacol. 2015;87(3):401-9. doi: 10.1124/mol.114.096693. Epub 2014 Dec 17. PubMed PMID: 25519838; PubMed Central PMCID: PMC4352586.
3: Larsen AP, Bentzen BH, Grunnet M. Differential effects of Kv11.1 activators on Kv11.1a, Kv11.1b and Kv11.1a/Kv11.1b channels. Br J Pharmacol. 2010 Oct;161(3):614-28. doi: 10.1111/j.1476-5381.2010.00897.x. PubMed PMID: 20880400; PubMed Central PMCID: PMC2990159.
4: Grunnet M, Abbruzzese J, Sachse FB, Sanguinetti MC. Molecular determinants of human ether-à-go-go-related gene 1 (hERG1) K+ channel activation by NS1643. Mol Pharmacol. 2011 Jan;79(1):1-9. doi: 10.1124/mol.110.067728. Epub 2010 Sep 27. PubMed PMID: 20876384; PubMed Central PMCID: PMC3014275.
5: Abbruzzese J, Sachse FB, Tristani-Firouzi M, Sanguinetti MC. Modification of hERG1 channel gating by Cd2+. J Gen Physiol. 2010 Aug;136(2):203-24. doi: 10.1085/jgp.201010450. PubMed PMID: 20660661; PubMed Central PMCID: PMC2912066.
6: Perry M, Sachse FB, Abbruzzese J, Sanguinetti MC. PD-118057 contacts the pore helix of hERG1 channels to attenuate inactivation and enhance K+ conductance. Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20075-80. doi: 10.1073/pnas.0906597106. Epub 2009 Nov 5. PubMed PMID: 19892732; PubMed Central PMCID: PMC2785294.
7: Perry M, Sanguinetti MC. A single amino acid difference between ether-a-go-go- related gene channel subtypes determines differential sensitivity to a small molecule activator. Mol Pharmacol. 2008 Apr;73(4):1044-51. Epub 2007 Dec 27. PubMed PMID: 18162604; PubMed Central PMCID: PMC2517227.
8: Perry M, Sachse FB, Sanguinetti MC. Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator. Proc Natl Acad Sci U S A. 2007 Aug 21;104(34):13827-32. Epub 2007 Aug 10. PubMed PMID: 17693551; PubMed Central PMCID: PMC1959467.
9: Zhou J, Augelli-Szafran CE, Bradley JA, Chen X, Koci BJ, Volberg WA, Sun Z, Cordes JS. Novel potent human ether-a-go-go-related gene (hERG) potassium channel enhancers and their in vitro antiarrhythmic activity. Mol Pharmacol. 2005 Sep;68(3):876-84. Epub 2005 Jun 23. PubMed PMID: 15976038.
10: Seebohm G. Activators of cation channels: potential in treatment of channelopathies. Mol Pharmacol. 2005 Mar;67(3):585-8. Epub 2004 Dec 17. Review. PubMed PMID: 15608141.
11: Kang J, Chen XL, Wang H, Ji J, Cheng H, Incardona J, Reynolds W, Viviani F, Tabart M, Rampe D. Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Mol Pharmacol. 2005 Mar;67(3):827-36. Epub 2004 Nov 17. PubMed PMID: 15548764.
