Propafenone HCl 具有抗心律不齐的功效,可用于心房和心室性心律不齐。
产品描述
Propafenone HCl is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias.
体外活性
MK 3207 exhibits significantly higher affinity for both native and recombinant human CGRP receptor, as well as rhesus monkey CGRP receptor with Ki of 24 pM, ~24 pM and 22 pM, respectively, as compared to CGRP receptors from other species, including canine and rodent (Ki values of ~10 nM). Although has affinity for AMY1 (CTR/RAMP1) receptor with a Ki value of 0.75 nM, MK 3207 displays marked selectivity for human CGRP receptor versus related human AM1 (CLR/RAMP2) receptor, AM2 (CLR/RAMP3) receptor, AMY3 (CTR/RAMP3) receptor, and CTR with Ki values of 16.5 μM, 0.156 μM, 0.128 μM and 1.9 μM, respectively. MK 3207 potently inhibits human α-CGRP-induced cAMP production in HEK293 cells stably expressing human CLR/RAMP1 with an IC50 of 0.12 nM, and maintains similar potency in the presence of 50% human serum with an IC50 of 0.17 nM, indicating that the activity of MK 3207 would not be dramatically affected by plasma protein binding in vivo. MK 3207 exhibits approximately 65-fold more potent in the human serum-shifted in vitro functional assay than telcagepant with an IC50 of 10.9 nM. [1]
Cas No.
34183-22-7
分子式
C21H28ClNO3
分子量
377.91
别名
Arythmol;Rythmol;Rytmonorm;Propafenone HCl;盐酸普罗帕酮;SA-79 (hydrochloride)
储存和溶解度
H2O:<1 mgml
Ethanol:<1 mgml
DMSO:64 mg/mL (169.4 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years