Membrane Transporters/Ion Channels
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CFTR activator
VX-770 (Ivacaftor)被称为CFTR增强剂，靶向作用于G551D-CFTR和F508del-CFTR，在fisher大鼠甲状腺细胞中EC50分别为100 nM和25 nM。
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- Okiyoneda T, .et al. Chaperone-Independent Peripheral Quality Control of CFTR by RFFL E3 Ligase, Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
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Myosin activator
CK-1827452 (Omecamtiv mecarbil)是选择性的心脏特异性肌球蛋白激活剂。
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- Oleg Lookin, .et al. Omecamtiv mecarbil attenuates length-tension relationship in healthy rat myocardium and preserves it in monocrotaline-induced pulmonary heart failure, Clin Exp Pharmacol Physiol, 2021, Aug 29 PMID: 34459025
- Gabor A. Fulop, .et al. Omecamtiv mecarbil evokes diastolic dysfunction and leads to periodic electromechanical alternans, Basic Res Cardiol, 2021, 116(1): 24 PMID: 33844095
- Wanjian Tang, .et al. Dilated cardiomyopathy mutation in the converter domain of human cardiac myosin alters motor activity and response to omecamtiv mecarbil, J Biol Chem, 2019, October 2 PMID: 31578282
- Thinh T. Kieu, .et al. Omecamtiv Mecarbil Slows Myosin Kinetics in Skinned Rat Myocardium at Physiological Temperature, Biophysical Journal, 2019, 2019 PMID: 31103235
- Alexandre J. S. Ribeiro, .et al. Multi-Imaging Method to Assay the Contractile Mechanical Output of Micropatterned Human iPSC-Derived Cardiac Myocytes, Circ Res, 2017, May 12; 120(10): 1572-1583 PMID: 28400398
- Anja M. Swenson, .et al. Omecamtiv Mecarbil Enhances the Duty Ratio of Human β-Cardiac Myosin Resulting in Increased Calcium Sensitivity and Slowed Force Development in Cardiac Muscle, J Biol Chem, 2017, Mar 3; 292(9): 3768-3778 PMID: 28082673
- Nánási P Jr, .et al. Omecamtiv mecarbil activates ryanodine receptors from canine cardiac but not skeletal muscle, Eur J Pharmacol, 2017, Aug 15;809:73-79 PMID: 28506910
- Horv??th B, .et al. Frequency-dependent effects of omecamtiv mecarbil on cell shortening of isolated canine ventricular cardiomyocytes, Naunyn Schmiedebergs Arch Pharmacol, 2017, Dec;390(12):1239-1246 PMID: 28940010
- Szentandrassy N, .et al. Dose-dependent electrophysiological effects of the myosin activator omecamtiv mecarbil in canine ventricular cardiomyocytes, J Physiol Pharmacol, 2016, Aug;67(4):483-489 PMID: 27779469
- L Nagy, .et al. The novel cardiac myosin activator omecamtiv mecarbil increases the calcium sensitivity of force production in isolated cardiomyocytes and skeletal muscle fibres of the rat, Br J Pharmacol, 2015, Sep; 172(18): 4506-4518 PMID: 26140433
- Larissa Butler, .et al. Enhanced characterization of contractility in cardiomyocytes during early drug safety assessment, Toxicol Sci, 2015, Jun;145(2):396-406 PMID: 25820236
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Calcium Channel Activator
Bay K 8644是一种有效的L型Ca2+通道选择性激活剂，IC50为17.3 nM。
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KCNQ1 potassium channel activator
ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.
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hERG channel activator
NS-1643是一种人类以太相关基因（hERG）KV11.1通道激活剂（EC50 = 10.5 uM）。
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HERG activator
RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.
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Kir6 (KATP) channel opener
Nicorandil (SG-75) 钾离子通道活化剂。
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KCa3.1 channel activator
NS 309是小和中电导Ca2+激活的K+通道（KCa2和KCa3.1通道）的正调制器。
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KCa2.1 channels activator
GW 542573X是小电导Ca2+激活的K+通道（KCa2）的激活剂。
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potassium channel activator
SKA-31是KCa2和KCa3.1钙激活钾通道的激活剂。
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KV7.2/7.3 activator
ICA-110381是KV7.2/7.3激活剂，EC50为0.38 uM。
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Potassium channel activator
NS1619是Bkca开启剂或大电导Ca2+激活的钾（BKCa，KCa1.1）通道激活剂。
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hERG1 potassium channel activator
KB130015是hERG1钾离子通道的新型激活剂，可在高压下阻断天然和重组hERG1通道，但在低压下激活它们。
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K+ (KATP) channel activator
Y-26763 is a K+ channel opener and active metabolite of Y-27152. Y-26763 is an ATP-sensitive K+ (KATP) channel activator.
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CaCC activator
Eact激活钙激活的氯离子通道（CaCC）TMEM16A CaCC。
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TRPML3 ion channel activator
SN 2 is a novel and potent activator of TRPML3 ion channel with EC50 of 1.8??0.13 μM.
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TRPM8 and TRPA1 activator
Icilin是一种冷却剂，可激活新型的冷受体TRPM8（CMR1）和TRPA1（ANKTM1/TRPN1），它们是TRP离子通道家族的成员。在表达CMR1的HEK 293细胞中感应电流（EC50 = 0.36μM）。
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TRPA1 activatior/TRPM8 blocker
Cannabichromene是一种主要的非精神植物大麻素，可抑制内源性大麻素失活并激活瞬时受体电位锚蛋白1（TRPA1）。内源性大麻素和TRPA1均可调节肠胃蠕动。
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photoactive TRPA1 activator
Optovin是可逆光敏trpa1活化剂。
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TRPV4 Activator
GSK1016790A是一种新型有效的TRPV4激活剂（瞬态受体电位香草酸4），在脉络丛上皮细胞中的EC50为34nM。
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Oct4 activator
OAC2是一种Oct4激活化合物，可通过Oct4基因启动子激活表达。
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Oct4 Activator
OAC1通过增强Oct4和Nanog驱动的基因表达来增强iPSC重编程效率。
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