Potassium Channel

Potassium Channel相关产品(91)
货号 产品名 中文名称 产品描述
SJ-MX0225 H3B-120

H3B-120 是一种高选择性,竞争性和变构的氨基甲酰磷酸合成酶 1(carbamoyl phosphate synthetase 1, CPS1) 变构抑制剂,可在氨基甲酰磷酸合成的第一步中阻断 ATP 水解,其IC50值为1.5 μM,其Ki值为1.4 μM。H3B-120可以限制高表达CPS1的癌细胞的嘧啶生物合成,从而表现出抗肿瘤活性。

SJ-MA0064 Nigericin sodium salt 尼日利亚菌素钠盐

Nigericin sodium salt 是从吸水链霉菌中得到的一种抗生素,作为 H+,K+ 和 Pb2+ 离子载体起作用,NLRP3 的激动剂。

SJ-MX2740 NS-1619

NS 1619 是选择性大电导 Ca 2+ 激活的 K + 通道激活剂。NS 1619 对心肌缺血再灌注损伤具有保护作用。

SJ-MX2829 Vernakalant hydrochloride 盐酸维那卡兰 Vernakalant hydrochloride, formerly known as RSD1235, is an investigational drug for the acute conversion of atrial fibrillation. Like other class III antiarrhythmics, vernakalant blocks atrial potassium channels, thereby prolonging repolarization. It differs from typical class III agents by blocking a certain type of potassium channel, the cardiac transient outward potassium current, with increased potency as the heart rate increases. This means that it is more effective at high heart rates, while other class III agents tend to lose effectiveness under these circumstances. It also slightly blocks the hERG potassium channel, leading to a prolonged QT interval. Vernakalant also blocks atrial sodium channels.
SJ-MX2843 E-4031 E-4031是III类抗心律失常药,选择性地阻断hERG钾通道。
SJ-MX2894 ML133 hydrochloride ML133 hydrochloride is an inward-rectifier potassium channel 2 (Kir2) inhibitor. It inhibits Kir2.1 with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5. It is selective for Kir2 channels over Kir1.1 and Kir4.1 channels (IC50 values of 300 and 76 µM, respectively). ML133 inhibits the development of dynamic, but not punctate, mechanical allodynia in a mouse model of spared nerve injury.
SJ-MX3586 NS6180 NS6180 is a potent KCa3.1 channel blocker with nanomolar potency.
SJ-MX3712 ML402 ML402 is a potent and selective activator of TREK-1/-2 and an agonist for OPRM1-OPRD1 (OPRM1: opioid receptor mu 1; OPRD1: delta opioid receptor) heterdimerization. ML335 selectively activates OPRM1-OPRD1 heterodimerization which may have potential use in the treatment of pain and alleviate unwanted effects associated with opiate use. ML402-define a cryptic binding pocket unlike other ion channel small-molecule binding sites and, together with functional studies, identify a cation-π interaction that controls selectivity. Together, our data reveal a druggable K2P site that stabilizes the C-type gate 'leak mode' and provide direct evidence for K2P selectivity filter gating.Heteromerization of OPRM1 with OPRD1 leads to the modulation of receptor binding and signaling properties. It has further been shown that the selective activation of the OPRM1-OPRD1 heteromer by a combination of OPRM1 agonist with OPRD1 antagonist can be blocked by antibodies that selectively recognize the heteromer.
SJ-MX2993 APD668 APD668 is a potent and selective, orally active G protein-coupled receptor 119 agonist (EC50 values 2.7 nM and 23 nM for hGPR119 and rGPR119, respectively) with in vivo activity in rodent models of glucose control. APD 668 significantly improved blood glucose handling during glucose challenge in several diabetic and non-diabetic rodent models, showing a clear glucose-dependent effect on insulin release in a hyperglycemic clamp model in the Sprague–Dawley rat. APD 668 is not genotoxic, and shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki value 0.1 μM).
SJ-MX2475 PAP-1 PAP-1 (5-(4-Phenoxybutoxy)psoralen) 是一种有效的,选择性的,口服活性的 Kv1.3 阻滞剂 (EC50=2 nM)。PAP-1 以使用依赖性方式阻止 Kv1.3,并通过优先绑定到通道的 C 型灭活状态来起作用。PAP-1 比 Kv1.5 (EC50=45 nM) 表现出 23 倍的选择性,并且比所有其他 Kv1 家族通道表现出 3 3到 125 倍的选择性。PAP-1 不表现出细胞毒性或光毒性作用。
SJ-MX2655 Minoxidil 米诺地尔

米诺地尔是一种有效的小动脉血管扩张剂,一种抗高血压药。 米诺地尔的抗高血压活性是由于其硫酸盐代谢物米诺地尔硫酸盐。 在很大程度上,米诺地尔通过打开血管平滑肌细胞中对三磷酸腺苷敏感的钾通道起作用。 此外,米诺地尔通过促进头发生长和减少脱发来影响毛囊细胞。

SJ-MX1308A Oxybutynin chloride 盐酸奥昔布宁 Oxybutynin chloride 是一种抗胆碱能药,抑制血管 Kv 通道,IC50 为 11.51 μM。
SJ-MX1548 ML-297 ML 297 (VU 0456810) 是一种强效、选择性的 GIRK1/2 激活剂,EC50 值为 0.16 μM。ML 297 能用于癫痫病的研究。
SJ-MX2452 Retigabine (D-23129) 瑞替加滨 Retigabine (D-23129) 是一种新型的抗痉挛剂,在大范围的惊厥模型具有活性。其发挥活性的机制主要是开放神经元的KCNQ2-5电压门控钾离子通道。
SJ-MX2616 Glipizide 格列吡嗪 Glipizide is a antidiabetic; KATP channel blocker; the drug inhibits the sulfonylurea receptor 1 (SUR1), the regulatory subunit of the ATP-sensitive potassium channels (KATP) in pancreaticβcells.
SJ-MX2782 GW9508 GW9508 is a potent and selective agonist for the free fatty acid receptor FFA1 (GPR40).
SJ-MX2807 NS1643 NS1643 is a novel and potent human ether-a-go-go related gene (hERG) KV11 channel activator with EC50 of 10.5 μM. In Xenopus laevis oocytes, NS1643 increased both steady-state and tail current at all voltages tested. The EC(50) value for HERG channel activation was 10.5 microM. NS1643 also activates the ERG2 channel; however, the molecular mechanism of the activation differs between the ERG1 and ERG2 channels. For ERG2, NS1643 causes a left-ward shift of the activation curve, a faster time-constant of activation and a slower time-constant of inactivation as well as an increased relative importance for the fast component of deactivation to the total deactivation. In contrast, for ERG1, NS1643 causes a right-ward shift in the voltage-dependent release from inactivation but does not affect time-constants of deactivation.
SJ-MX2814 Nicorandil 尼可地尔 Nicorandil (formerly RP46417; SG-75; SG75; RP-46417; Dancor and Adancor) is a potassium channel activator that has been approved as a vasodilatory drug to treat angina. It stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP). Nicorandil causes vasodilatation of arterioles and large coronary arteries. Nicorandal's nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.
SJ-MX3736 Almitrine mesylate 甲磺酸阿米三嗪 Almitrine mesylate (marketed as Duxil by Servier) is a diphenylmethylpiperazine analogue classified as a respiratory stimulant by the ATC. It enhances respiration by acting as an agonist of peripheral chemoreceptors located on the carotid bodies. The drug increases arterial oxygen tension while decreasing arterial carbon dioxide tension in patients with chronic obstructive pulmonary disease. It may also prove useful in the treatment of nocturnal oxygen desaturation without impairing the quality of sleep.
SJ-MN0245 Daurisoline 蝙蝠葛苏林碱 Daurisoline 是一个 hERG 抑制剂,也是一种自噬抑制剂