Synonym
E 4080; E4080; E-4080;
IUPAC/Chemical Name
(E)-4-(4-(1H-imidazol-1-yl)phenyl)-N-(3-((3,5-dimethoxyphenethyl)(methyl)amino)propyl)but-3-enamide dihydrochloride
InChi Key
KKUNFGOKUGASRQ-SLNOCBGISA-N
InChi Code
InChI=1S/C27H34N4O3.2ClH/c1-30(16-12-23-18-25(33-2)20-26(19-23)34-3)15-5-13-29-27(32)7-4-6-22-8-10-24(11-9-22)31-17-14-28-21-31;;/h4,6,8-11,14,17-21H,5,7,12-13,15-16H2,1-3H3,(H,29,32);2*1H/b6-4+;;
SMILES Code
COc1cc(OC)cc(CCN(CCCNC(C/C=C/c2ccc(n3cncc3)cc2)=O)C)c1.Cl.Cl
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
>3 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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
535.51
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: Adachi H. Effects of E4080, a novel bradycardic agent with a coronary vasodilating property, on coronary and systemic hemodynamics in conscious dogs. J Pharmacol Exp Ther. 1994 Jan;268(1):133-8. PMID: 8301548.
2: Sawaki S, Furukawa Y, Inoue Y, Oguchi T, Chiba S. Selective inhibition by E4080, a novel bradycardic agent, of positive chronotropic responses to norepinephrine in isolated dog hearts. Eur J Pharmacol. 1993 Dec 7;250(2):253-9. doi: 10.1016/0014-2999(93)90389-y. PMID: 7509284.
3: Kodama K, Adachi H, Ogawa T, Ohhara H. Inhibitory effect of a novel antianginal agent, E4080, on ST segment elevation induced by vasopressin in anesthetized guinea pigs. Jpn J Pharmacol. 1992 Oct;60(2):73-7. doi: 10.1254/jjp.60.73. PMID: 1479745.
4: Okada Y, Yanagisawa T, Taira N. E4080 has a dual action, as a K+ channel opener and a Ca2+ channel blocker, in canine coronary artery smooth muscle. Eur J Pharmacol. 1992 Aug 6;218(2-3):259-64. doi: 10.1016/0014-2999(92)90177-6. PMID: 1330597.
5: Kamouchi M, Xiong Z, Teramoto N, Kajioka S, Okabe K, Kitamura K. Ionic currents involved in vasodilating actions of E4080, a newly synthesized bradycardia-inducing agent, in dispersed smooth muscle cells of the rabbit portal vein. J Pharmacol Exp Ther. 1991 Dec;259(3):1396-403. PMID: 1762086.
6: Kawamura T, Adachi H, Ogawa T. Cardiovascular effects of E4080, a novel bradycardiac agent with coronary vasodilating properties, in anesthetized dogs. Eur J Pharmacol. 1991 Oct 22;203(3):399-404. doi: 10.1016/0014-2999(91)90897-y. PMID: 1773825.
