| Chemical & Physical Properties | |
|---|---|
| CAS Number | 149888-94-8 |
| Catalog No. | 2A-1190704 |
| Chinese Name | 盐酸阿齐利特 |
| Synonyms | azmilide; Azimilide hydrochloride; Stedicor; Azimilide HCl; Azimilide dihydrochloride; Azimilide (Dihydrochloride) |
| Molecular Formula | C23H30O3N5Cl3 |
| Molecular Weight | 530.88 |
| Density | 1.32g/cm3 |
| Boiling Point | 594.9ºC at 760mmHg |
| Storage Condition | 2-8℃ |
| Application | Azimilide dihydrochloride (NE-10064) is an antiarrhythmic compound that inhibits I(Ks) and I(Kr) activity. |
| MDL Number | MFCD00918091 |
| SMILES | CN1CCN(CCCCN2C(=O)CN(N=Cc3ccc(-c4ccc(Cl)cc4)o3)C2=O)CC1.Cl.Cl |
| InChI | InChI=1S/C23H28ClN5O3.2ClH/c1-26-12-14-27(15-13-26)10-2-3-11-28-22(30)17-29(23(28)31)25-16-20-8-9-21(32-20)18-4-6-19(24)7-5-18;;/h4-9,16H,2-3,10-15,17H2,1H3;2*1H/b25-16+;; |
| InChI Key | HHPSICLSNHCSNZ-BYEGLACWSA-N |
| Hazard Symbols | transportation |
| Bioactivity | Azimilide 2Hcl(NE-10064 2Hcl) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.IC50 value:Target: in vitro: Azimilide blocked HERG channels at 0.1 and 1 Hz with IC50s of 1.4 microM and 5.2 microM respectively. Azimilide blockade of HERG channels expressed in Xenopus oocytes and I(Kr) in mouse AT-1 cells was decreased under conditions of high [K+]e, whereas block of slowly activating I(Ks) channels was not affected by changes in [K+]e [1]. Azimilide suppressed the following currents (Kd in parenthesis): IKr (< 1 microM at -20 mV), IKs (1.8 microM at +30 mV), L-type Ca current (17.8 microM at +10 mV), and Na current (19 microM at -40 mV). Azimilide was a weak blocker of the transient outward and inward rectifier currents (Kd > or = 50 microM at +50 and -140 mV, respectively). Azimilide blocked IKr, IKs, and INa in a use-dependent manner. Furthermore, azimilide reduced a slowly inactivating component of Na current that might be important for maintaining the action potential plateau in canine ventricular myocytes [2]. In guinea pig ventricular myocytes, NE-10064 (0.3-3 microM) significantly prolonged action potential duration (APD) at 1 Hz. At 3 Hz, NE-10064 (0.3-1 microM) increased APD only slightly, and at 10 microM decreased APD and the plateau potential. NE-10064 potently blocked the rapidly activating component of the delayed rectifier, IKr (IC50 0.4 microM), and inhibited IKs (IC50 3 microM) with nearly 10-fold less potency [3].in vivo: NE-10064 (10 mg/kg intravenously, i.v.) reduced (p < 0.05) the incidence (8 of 12) of PES-induced ventricular tachycardia (VT). The cycle length of induced VT was not prolonged by NE-10064 (0.245 ± 0.046 s predrug vs. 0.301 ± 0.060 s postdrug). NE-10064 increased ventricular effective refractory period (VERP 166 ± 5 ms predrug vs. 194 ± 13 ms postdrug, p = 0.013), prolonged QTc interval (310 ± 12 ms predrug vs. 350 ± 16 ms postdrug, p = 0.004) and prolonged the effective refractory period (ERP) of noninfarcted myocardium (p = 0.045) [4]. Related Catalog Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel Research Areas >> Cardiovascular Disease References [1]. Busch AE, et al. Blockade of HERG channels by the class III antiarrhythmic azimilide: mode of action. Br J Pharmacol. 1998 Jan;123(1):23-30. [2]. Yao JA, et al. Azimilide (NE-10064) can prolong or shorten the action potential duration in canine ventricular myocytes: dependence on blockade of K, Ca, and Na channels. J Cardiovasc Electrophysiol. 1997 Feb;8(2):184-98. [3]. Fermini B, et al. Use-dependent effects of the class III antiarrhythmic agent NE-10064 (azimilide) on cardiac repolarization: block of delayed rectifier potassium and L-type calcium currents. J Cardiovasc Pharmacol. 1995 Aug;26(2):259-71. [4]. Black SC, et al. Protection against programmed electrical stimulation-induced ventricular tachycardia and sudden cardiac death by NE-10064, a class III antiarrhythmic drug. J Cardiovasc Pharmacol. 1993 Dec;22(6):810-8. Chemical & Physical Properties Density 1.32g/cm3 Boiling Point 594.9ºC at 760mmHg Molecular Formula C23H30Cl3N5O3 Molecular Weight 530.87500 Flash Point 313.6ºC Exact Mass 529.14100 PSA 72.60000 LogP 4.58130 InChIKey HHPSICLSNHCSNZ-BYEGLACWSA-N SMILES CN1CCN(CCCCN2C(=O)CN(N=Cc3ccc(-c4ccc(Cl)cc4)o3)C2=O)CC1.Cl.Cl Storage condition 2-8℃ |
| Use of | Properties Articles27 Name 1-[(E)-[5-(4-chlorophenyl)furan-2-yl]methylideneamino]-3-[4-(4-methylpiperazin-1-yl)butyl]imidazolidine-2,4-dione,dihydrochloride Synonym More Synonyms Azimilide (Dihydrochloride) Biological Activity Related Catalog Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel Research Areas >> Cardiovascular Disease References [1]. Busch AE, et al. Blockade of HERG channels by the class III antiarrhythmic azimilide: mode of action. Br J Pharmacol. 1998 Jan;123(1):23-30. [2]. Yao JA, et al. Azimilide (NE-10064) can prolong or shorten the action potential duration in canine ventricular myocytes: dependence on blockade of K, Ca, and Na channels. J Cardiovasc Electrophysiol. 1997 Feb;8(2):184-98. [3]. Fermini B, et al. Use-dependent effects of the class III antiarrhythmic agent NE-10064 (azimilide) on cardiac repolarization: block of delayed rectifier potassium and L-type calcium currents. J Cardiovasc Pharmacol. 1995 Aug;26(2):259-71. [4]. Black SC, et al. Protection against programmed electrical stimulation-induced ventricular tachycardia and sudden cardiac death by NE-10064, a class III antiarrhythmic drug. J Cardiovasc Pharmacol. 1993 Dec;22(6):810-8. Chemical & Physical Properties Exact Mass 529.14100 PSA 72.60000 LogP 4.58130 InChIKey HHPSICLSNHCSNZ-BYEGLACWSA-N Storage condition 2-8℃ |
| Transport Info | Product name: Purity: 98.0% |
| MSDS Transport Info | Module 14. Shipping information European Dangerous Regulations for land transport: 2811 International Dangerous Regulations for sea transport: 2811 International Dangerous Regulations for air transport: 2811 14.2 Names specified by the United Nations (UN) European Land Transport Dangerous Regulations: TOXIC SOLID, ORGANIC, N.O.S. (Azimilide dihydrochloride) IMDG Code: TOXIC SOLID, ORGANIC, N.O.S. (Azimilide dihydrochloride) International air transport hazard regulations: Toxic solid, organic, n.o.s. (Azimilide dihydrochloride) 14.3 Transport hazard categories European Land Transport Danger Regulations: 6.1 International Maritime Transport Danger Regulations: 6.1 International Air Transport Danger Regulations: 6.1 14.4 Package group European Land Transport Danger Regulations: III International Maritime Transport Danger Regulations: III International Air Transport Danger Regulations: III 14.5 Environmental hazards European Land Transport Dangerous Regulations: No International Maritime Transport Dangerous Regulations Maritime Pollutants: No International Air Transport Risk Regulations: No 14.6 Special reminder to users No data available |
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