WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H528528
CAS#: 104606-13-5
Description: R-56865 is a calcium and sodium channel antagonist potentially for the treatment of arrhythmias and ischaemic heart disorders. R-56865 showed marked cardioprotective properties: in the reperfusion period the agent markedly improved the restoration of left ventricular developed pressure, ATP and phosphocreatine, furthermore contracture development was reduced. On hypoxic cells, R-56865 selectively reduced the amplitude of hypoxia-induced membrane depolarization and partly counteracted the depression of synaptic transmission evoked by Schaffers collateral stimulation.
Hodoodo Cat#: H528528
Name: R-56865
CAS#: 104606-13-5
Chemical Formula: C23H28FN3OS
Exact Mass: 413.19
Molecular Weight: 413.555
Elemental Analysis: C, 66.80; H, 6.82; F, 4.59; N, 10.16; O, 3.87; S, 7.75
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Synonym: R-56865; R 56865; R56865
IUPAC/Chemical Name: N-(1-(4-(4-fluorophenoxy)butyl)piperidin-4-yl)-N-methylbenzo[d]thiazol-2-amine
InChi Key: PZPXREFPAFDHNG-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H28FN3OS/c1-26(23-25-21-6-2-3-7-22(21)29-23)19-12-15-27(16-13-19)14-4-5-17-28-20-10-8-18(24)9-11-20/h2-3,6-11,19H,4-5,12-17H2,1H3
SMILES Code: CN(C1CCN(CCCCOC2=CC=C(F)C=C2)CC1)C3=NC4=CC=CC=C4S3
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 413.56 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: Wang L, Lopaschuk GD, Clanachan AS. H(2)O(2)-induced left ventricular dysfunction in isolated working rat hearts is independent of calcium accumulation. J Mol Cell Cardiol. 2008 Dec;45(6):787-95. doi: 10.1016/j.yjmcc.2008.08.010. Epub 2008 Sep 6. PubMed PMID: 18817782.
2: Kim YC, Sim JH, Kang TM, Suzuki H, Kim SR, Kwon SC, Xu WX, Lee SJ, Kim KW. Sodium-activated potassium current in guinea pig gastric myocytes. J Korean Med Sci. 2007 Feb;22(1):57-62. PubMed PMID: 17297252; PubMed Central PMCID: PMC2693569.
3: Létienne R, Vié B, Le Grand B. Pharmacological characterisation of sodium channels in sinoatrial node pacemaking in the rat heart. Eur J Pharmacol. 2006 Jan 20;530(3):243-9. Epub 2005 Dec 20. PubMed PMID: 16368090.
4: Hartmann M, Decking UK. R 56865 exerts cardioprotective properties independent of the intracellular Na(+)-overload in the guinea pig heart. Naunyn Schmiedebergs Arch Pharmacol. 2003 Sep;368(3):160-5. Epub 2003 Sep 2. PubMed PMID: 14513202.
5: Li Y, Sato T, Arita M. Bepridil blunts the shortening of action potential duration caused by metabolic inhibition via blockade of ATP-sensitive K(+) channels and Na(+)-activated K(+) channels. J Pharmacol Exp Ther. 1999 Nov;291(2):562-8. PubMed PMID: 10525072.
6: Barbieri M, Nistri A. Electrophysiological actions of N-[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]-N-methyl-2-benzothiazola mine (R56865) on CA1 neurons of the rat hippocampal slice during hypoxia. Neurosci Lett. 1999 Aug 6;270(3):161-4. PubMed PMID: 10462119.
7: Lawrence C, Rodrigo GC. A Na+-activated K+ current (IK,Na) is present in guinea-pig but not rat ventricular myocytes. Pflugers Arch. 1999 May;437(6):831-8. PubMed PMID: 10370060.
8: Ravens U, Himmel HM. Drugs preventing Na+ and Ca2+ overload. Pharmacol Res. 1999 Mar;39(3):167-74. Review. PubMed PMID: 10094840.
9: Adachi Y, Suzuki Y, Homma N, Fukazawa M, Tamura K, Nishie I, Kuromaru O. The anti-ischemic effects of CP-060S during pacing-induced ischemia in anesthetized dogs. Eur J Pharmacol. 1999 Feb 19;367(2-3):267-73. PubMed PMID: 10079001.
10: Lu HR, Yang P, Remeysen P, Saels A, Dai DZ, De Clerck F. Ischemia/reperfusion-induced arrhythmias in anaesthetized rats: a role of Na+ and Ca2+ influx. Eur J Pharmacol. 1999 Jan 22;365(2-3):233-9. PubMed PMID: 9988107.
11: Le Grand B, Coulombe A, John GW. Late sodium current inhibition in human isolated cardiomyocytes by R 56865. J Cardiovasc Pharmacol. 1998 May;31(5):800-4. PubMed PMID: 9593082.
12: Koga T, Fukazawa M, Suzuki Y, Akima M, Adachi Y, Tamura K, Kato T, Kuromaru O. The protective effects of CP-060S on ischaemia- and reperfusion- induced arrhythmias in anaesthetized rats. Br J Pharmacol. 1998 Apr;123(7):1409-17. PubMed PMID: 9579737; PubMed Central PMCID: PMC1565298.
13: De la Fuente MT, Maroto R, Esquerro E, Sánchez-García P, García AG. The actions of ouabain and lithium chloride on cytosolic Ca2+ in single chromaffin cells. Eur J Pharmacol. 1996 Jun 13;306(1-3):219-26. PubMed PMID: 8813635.
14: Ishide N. Intracellular calcium modulators for cardiac muscle in pathological conditions. Jpn Heart J. 1996 Jan;37(1):1-17. Review. PubMed PMID: 8632617.
15: Thollon C, Iliou JP, Cambarrat C, Robin F, Vilaine JP. Nature of the cardiomyocyte injury induced by lipid hydroperoxides. Cardiovasc Res. 1995 Nov;30(5):648-55. PubMed PMID: 8595608.
16: Swan GE, Schultz RA, Kellerman TS, Mülders MS, Maartens BP, Van der Walt JJ. In vivo effects of a novel calcium antagonist (R56865) against induced epoxyscillirosidin and tulp poisoning in sheep. Onderstepoort J Vet Res. 1995 Sep;62(3):163-6. PubMed PMID: 8628568.
17: Scheufler E, Mozes A, Guttmann I, Wilffert B. R56865 is antifibrillatory in reperfused ischemic guinea-pig hearts, even when given only during reperfusion. Cardiovasc Drugs Ther. 1995 Aug;9(4):545-53. PubMed PMID: 8547204.
18: Le Grand B, Vie B, Talmant JM, Coraboeuf E, John GW. Alleviation of contractile dysfunction in ischemic hearts by slowly inactivating Na+ current blockers. Am J Physiol. 1995 Aug;269(2 Pt 2):H533-40. PubMed PMID: 7653617.
19: Park SR, Ryu GH, Suh CK. Cardioprotective drugs decrease the Na+ background current. Yonsei Med J. 1995 Jul;36(3):278-86. PubMed PMID: 7660679.
20: Xie Y, Zacharias E, Hoff P, Tegtmeier F. Ion channel involvement in anoxic depolarization induced by cardiac arrest in rat brain. J Cereb Blood Flow Metab. 1995 Jul;15(4):587-94. PubMed PMID: 7540620.
