Synonym
Lidoflazine; Ordiflazine; Clinium; Corflazine; Klinium;
IUPAC/Chemical Name
2-[4-[4,4-Bis(4-fluorophenyl)butyl]piperazin-1-yl]-N-(2,6-dimethylphenyl)acetamide
InChi Key
ZBIAKUMOEKILTF-UHFFFAOYSA-N
InChi Code
InChI=1S/C30H35F2N3O/c1-22-5-3-6-23(2)30(22)33-29(36)21-35-19-17-34(18-20-35)16-4-7-28(24-8-12-26(31)13-9-24)25-10-14-27(32)15-11-25/h3,5-6,8-15,28H,4,7,16-21H2,1-2H3,(H,33,36)
SMILES Code
O=C(NC1=C(C)C=CC=C1C)CN2CCN(CCCC(C3=CC=C(F)C=C3)C4=CC=C(F)C=C4)CC2
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
Biological target:
Lidoflazine is a high affinity blocker of the HERG (human ether-a-go-go-related gene) K+ channel.
In vitro activity:
Lidoflazine inhibited potently HERG current (I(HERG)) recorded from HEK 293 cells stably expressing wild-type HERG (IC(50) of approximately 16 nM). It was approximately 13-fold more potent against HERG than was verapamil under similar conditions.
Reference: J Mol Cell Cardiol. 2004 May;36(5):701-5. https://pubmed.ncbi.nlm.nih.gov/15135665/
In vivo activity:
The effects of pretreatment with the nucleoside transport inhibitor lidoflazine on repeated ischemia-reperfusion injury induced by normothermic intermittent aortic crossclamping were studied in canine hearts. In the lidoflazine group, myocardial adenosine content (0.25 +/- 0.06 mumol/gm dry weight) was 3.5 times higher than that in the control group (0.07 +/- 0.03 mumol/gm dry weight; p < 0.05) at the end of the last aortic crossclamping.
Reference: J Thorac Cardiovasc Surg. 1992 Dec;104(6):1602-9. https://pubmed.ncbi.nlm.nih.gov/1453724/
Preparing Stock Solutions
The following data is based on the
product
molecular weight
491.63
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:
1. Ridley JM, Dooley PC, Milnes JT, Witchel HJ, Hancox JC. Lidoflazine is a high affinity blocker of the HERG K(+)channel. J Mol Cell Cardiol. 2004 May;36(5):701-5. doi: 10.1016/j.yjmcc.2004.02.009. PMID: 15135665.
2. Hart G, Dukes ID. An analysis of the rate-dependent action of lidoflazine in mammalian sino-atrial node and Purkinje fibres. J Mol Cell Cardiol. 1984 Jan;16(1):33-42. doi: 10.1016/s0022-2828(84)80712-9. PMID: 6699917.
3. Chang-Chun C, Masuda M, Szabò Z, Szerafin T, Szècsi J, Van Belle H, Flameng W. Nucleoside transport inhibition mediates lidoflazine-induced cardioprotection during intermittent aortic crossclamping. J Thorac Cardiovasc Surg. 1992 Dec;104(6):1602-9. PMID: 1453724.
4. Guvendik L, Hynd J, Drake-Holland A, Parker DJ. Myocardial protective effects of lidoflazine during ischemia and reperfusion. Thorac Cardiovasc Surg. 1990 Feb;38(1):15-9. doi: 10.1055/s-2007-1013984. PMID: 2309223.
In vitro protocol:
1. Ridley JM, Dooley PC, Milnes JT, Witchel HJ, Hancox JC. Lidoflazine is a high affinity blocker of the HERG K(+)channel. J Mol Cell Cardiol. 2004 May;36(5):701-5. doi: 10.1016/j.yjmcc.2004.02.009. PMID: 15135665.
2. Hart G, Dukes ID. An analysis of the rate-dependent action of lidoflazine in mammalian sino-atrial node and Purkinje fibres. J Mol Cell Cardiol. 1984 Jan;16(1):33-42. doi: 10.1016/s0022-2828(84)80712-9. PMID: 6699917.
In vivo protocol:
1. Chang-Chun C, Masuda M, Szabò Z, Szerafin T, Szècsi J, Van Belle H, Flameng W. Nucleoside transport inhibition mediates lidoflazine-induced cardioprotection during intermittent aortic crossclamping. J Thorac Cardiovasc Surg. 1992 Dec;104(6):1602-9. PMID: 1453724.
2. Guvendik L, Hynd J, Drake-Holland A, Parker DJ. Myocardial protective effects of lidoflazine during ischemia and reperfusion. Thorac Cardiovasc Surg. 1990 Feb;38(1):15-9. doi: 10.1055/s-2007-1013984. PMID: 2309223.
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