RPR260243 | CAS#668463-35-2 |HERG Activator

MedKoo Cat#: 532579 | Name: RPR260243

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

RPR260243

CAS#668463-35-2

Theoretical Analysis

MedKoo Cat#: 532579

Name: RPR260243

CAS#: 668463-35-2

Chemical Formula: C28H25F3N2O4

Exact Mass: 510.1766

Molecular Weight: 510.51

Elemental Analysis: C, 65.88; H, 4.94; F, 11.16; N, 5.49; O, 12.54

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

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

Instruction

View handling instruction

Preparing Stock Solutions

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

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.