WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H463281
CAS#: 127404-34-6
Description: E 4080 is a novel bradycardic agent with a coronary vasodilating property.
Hodoodo Cat#: H463281
Name: E 4080
CAS#: 127404-34-6
Chemical Formula: C27H36Cl2N4O3
Exact Mass: 534.22
Molecular Weight: 535.510
Elemental Analysis: C, 60.56; H, 6.78; Cl, 13.24; N, 10.46; O, 8.96
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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
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: >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
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
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.