SML2354
HMR-1556
≥98% (HPLC), KCNQ1-KCNE1 (KvLQT1-MinK) blocker, powder
别名:
(3R,4S)-(+)-N-[3-Hydroxy-2,2-dimethyl-6-(4,4,4,-trifluorobutoxy)chroman-4-yl]-N-methylmethanesulfonamide, Chromanol HMR 1556, HMR 1556, HMR1556, N-[(3R,4S)-3,4-Dihydro-3-hydroxy-2,2-dimethyl-6-(4,4,4-trifluorobutoxy)-2H-1-benzopyran-4-yl]-N-methylmethanesulfonamide
产品名称
HMR-1556, ≥98% (HPLC)
方案
≥98% (HPLC)
表单
powder
旋光性
[α]/D +2 to +3.5°, c = 0.1 in methanol
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
CC1([C@@H]([C@H](C2=CC(OCCCC(F)(F)F)=CC=C2O1)N(C)S(C)(=O)=O)O)C
InChI
1S/C17H24F3NO5S/c1-16(2)15(22)14(21(3)27(4,23)24)12-10-11(6-7-13(12)26-16)25-9-5-8-17(18,19)20/h6-7,10,14-15,22H,5,8-9H2,1-4H3/t14-,15+/m0/s1
InChI key
SRZRLJWUQFIZRH-LSDHHAIUSA-N
相关类别
生化/生理作用
HMR-1556 is a potent and selective blocker of the heteromeric KCNQ1-KCNE1 (KvLQT1-MinK) voltage-gated channel-mediated slowly activating K+ current (IKs IC50 = 120 nM in hKCNE1-transfected Xenopus oocytes; little or no inhibition of Herg, Kv1.3 (KCNA3), Kv1.5 (KCNA5), Kir2.1 (KCNJ2), HCN2 (BCNG2) current in respective oocyte transfectants). HMR-1556 is more potent than chromanol 293B (IKs IC50 = 34 nM and 2.1 μM, respectively; guinea pig ventricular myocytes), being inefficient against L-type Ca2+ channel or rapidly delayed & inward rectifier currents (IKr & IK1) in guinea pig ventricular myocytes, nor transient & sustained outward currents, I(to) & I(sus), in rat ventricular myocytes.
Potent and selective blocker of the heteromeric KCNQ1-KCNE1 (KvLQT1-MinK) voltage-gated channel-mediated slowly activating K+ current (Iks).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
U Gerlach et al.
Journal of medicinal chemistry, 44(23), 3831-3837 (2001-11-02)
Since the discovery of the I(Ks)-potassium channel as the slowly activating component of the delayed rectifier current (I(k)) in cardiac tissue, the search for blockers of this current has been intense. During the screening of K(ATP)-channel openers of the chromanol
H Gögelein et al.
Naunyn-Schmiedeberg's archives of pharmacology, 362(6), 480-488 (2001-01-04)
Chromanol HMR 1556 [(3R,4S)-(+)-N-[3-hydroxy-2,2-dimethyl-6-(4,4,4-trifluorobutoxy)chroman-4-yl]-N-methylmethanesulfonamide], a novel inhibitor of the slow component of the delayed outward current in heart muscle cells (IKs), has been characterized in several in-vitro systems. mRNA encoding for the human protein minK was injected into Xenopus oocytes
James Winter et al.
Frontiers in physiology, 9, 16-16 (2018-02-08)
Rationale: Arrhythmogenic cardiac alternans are thought to be an important determinant for the initiation of ventricular fibrillation. There is limited information on the effects of sympathetic nerve stimulation (SNS) on alternans in the intact heart and the conclusions of existing
Ralph F Bosch et al.
Naunyn-Schmiedeberg's archives of pharmacology, 367(3), 281-288 (2003-03-20)
The chromanol HMR 1556 is a potent blocker of KvLQT1/minK potassium channels expressed in Xenopus oocytes. The compound is therefore a new class III antiarrhythmic drug with a distinct mechanism of action. However, the effect of HMR 1556 on atrial
Daniel C Bartos et al.
The Journal of physiology, 595(7), 2253-2268 (2016-12-23)
[Ca2+ ]i enhanced rabbit ventricular slowly activating delayed rectifier K+ current (IKs ) by negatively shifting the voltage dependence of activation and slowing deactivation, similar to perfusion of isoproterenol. Rabbit ventricular rapidly activating delayed rectifier K+ current (IKr ) amplitude
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