Membrane Transporters/Ion Channels
-
Calcium Channel 抑制剂
Nimodipine是一种L型Ca2+通道阻滞剂。
了解更多
-
Selective calcium chelator
BAPTA tetrapotassium是一种选择性钙螯合剂,对Ca2+的亲和力大于Mg2+。
了解更多
-
Selective calcium chelator
BAPTA/AM是一种细胞内钙螯合剂,可通过脂氧合酶介导的自由基在小鼠皮层培养物中诱导延迟性坏死。
了解更多
- Liying Wu, .et al. Capsaicin inhibits the stemness of anaplastic thyroid carcinoma cells by triggering autophagy-lysosome mediated OCT4A degradation, Phytother Res, 2022, Feb;36(2):938-950 PMID: 35076979
- Shichen Xu, .et al. Capsaicin induces mitochondrial dysfunction and apoptosis in anaplastic thyroid carcinoma cells via TRPV1-mediated mitochondrial calcium overload, Cell Signal, 2020, Aug 6;75:109733 PMID: 32771398
- Miho Akimoto, .et al. Antidiabetic adiponectin receptor agonist AdipoRon suppresses tumour growth of pancreatic cancer by inducing RIPK1/ERK-dependent necroptosis, Cell Death Dis, 2018, Aug; 9(8): 804 PMID: 30038429
- Zhang L, .et al. Curcumin induces endoplasmic reticulum stress-associated apoptosis in human papillary thyroid carcinoma BCPAP cells via disruption of intracellular calcium homeostasis, Medicine (Baltimore), 2018, Jun;97(24):e11095 PMID: 29901626
-
Ca2+ release 抑制剂
Dantrolene是一种肌肉松弛剂,其作用可能是通过消除对ryanodine受体的作用来消除肌肉细胞中的兴奋-收缩偶联。
了解更多
-
Atagabalin与加巴喷丁相关,加巴喷丁同样与α结合。2β钙通道(1和2)。
了解更多
-
-
Calcium channel blocker
(S)-Amlodipine是氨氯地平的(S)-对映体,具有活性的二氢吡啶钙通道阻滞剂主要存在于(-)-异构体中。
了解更多
-
Calcium channel blocker
NNC 55-0396是Mibefradil衍生物,是一种高度选择性的T型钙通道阻滞剂;分别在INS-1细胞中抑制Cav3.1 T型通道和HVA电流的IC50值为6.8和> 100μM。
了解更多
-
N-type calcium channel blocker
NP118809是有效的N型钙通道阻滞剂(IC50 = 0.11 uM);对L型钙通道的选择性好。
了解更多
-
K(Ca) 3.1 channel blocker
NS6180是一种新型有效的选择性KCa3.1通道抑制剂(IC50 = 9 nM),可防止T细胞活化和炎症反应。
了解更多
-
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。
了解更多
-
Calcium channel blocker
Mibefradil dihydrochloride是钙通道阻滞剂,对T型Ca2+通道具有中等选择性,对T型和L型通道的IC50值分别为2.7 uM和18.6 uM。
了解更多
-
Dantrolene sodium是一种骨骼肌松弛剂,其通过干扰肌肉纤维中的激发-收缩偶联起作用。
了解更多
-
CRAC channel 抑制剂
YM-58483是CRAC通道和随后的Ca2+信号的第一个选择性抑制剂。
了解更多
-
Chlorocresol是ryanodine受体的活化剂。
了解更多
-
Cinepazide maleate是Cinepazide的马来酸盐形式,其为血管扩张剂。
了解更多
-
calcium channel blocker
Cinnarizine是哌嗪的药物衍生物,其特征在于抗组胺药和钙通道阻滞剂。
了解更多
-
Calcium channel antagonist
Aranidipine (MPC1304) is a Ca2+ channel antagonist with potent and long-lasting antihypertensive effects.
了解更多
-
T-type Ca2+ channel blocker
ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
了解更多
-
Ca2+ channel agonist/CDK2 inhibitor
Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
了解更多
-
L-type calcium antagonist
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors.
了解更多
-
Calcium channel proteins inhibitor
Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm. Dantrolene sodium is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction.
了解更多
-
intracellular Ca2+ handling modulator
Caldaret is an intracellular Ca2+ handling modulator that acts through reverse mode Na+/Ca2+ exchanger inhibition.
了解更多
-
T-type Ca2+ channel blocker
ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
了解更多
-
L-type Ca2+ channel agonist
(S)-(-)-Bay-K-8644 is an agonist of L-type Ca2+ channel. (S)-(-)-Bay-K-8644 activates Ba2+ currents (IBa) (EC50=32 nM).
了解更多
-
T-type Ca2+ channel antagonist
TTA-Q6 is a selective T-type Ca2+ channel antagonist, used in the neurological disease.
了解更多
-
T-type Ca2+ channel antagonist
TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca2+ channel antagonist.
了解更多
-
Ca2+-dependent blocker
TV-519 free base (K201 free base) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
了解更多
-
N- and P/Q-type Ca2+ channels agonist
GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.
了解更多
-
CFTR 抑制剂
Oridonin (Isodonol)是一种从鼠李木中分离出来的Entkaurane二萜类化合物,是一种重要的传统中草药。
了解更多
-
CFTR 抑制剂
CFTRinh-172是电压无关的选择性CFTR抑制剂。在2分钟内可逆地抑制CFTR短路电流的 Ki 值为300 nM。
了解更多
- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
-
F508del-CFTR trafficking corrector
KM 11060纠正了F508del-CFTR的运输,增加了质膜上功能性CFTR的量(?75%)并抑制了PDE5的活性。
了解更多
-
CFTR potentiator
PG 01 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. PG 01 is effective on G970R although with a significant decrease in potency relative to E193K and δF508.
了解更多
-
CFTR corrector
CFTR corrector 2 is a cystic fibrosis transmembrane conductance corrector (CFTR), extracted from patent US20140274933.
了解更多
-
CFTR potentiator
GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC50 of 11.1 nM.
了解更多
-
CFTR potentiator
Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
了解更多
-
CFTR potentiator
Ivacaftor hydrate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
了解更多
-
CFTR 抑制剂
PTC124也称为Ataluren,是CFTR-G542X无意义等位基因抑制剂。
了解更多
- L Kadunc, .et al. Increased Gene Translation Stringency in Mammalian Cells by Nonsense Suppression at Multiple Permissive Sites With a Single Noncanonical Amino Acid, FEBS Lett, 2020, May 13 PMID: 32401336
- Caspi M, .et al. A flow cytometry-based reporter assay identifies macrolide antibiotics as nonsense mutation read-through agents, J Mol Med (Berl), 2016, Apr;94(4):469-82 PMID: 26620677
-
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。
了解更多
- 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
-
CFTR modulator
VX-809 (Lumacaftor)是用于治疗囊性纤维化(CF)的第二种口服研究候选化合物,通过促进突变型CFTR(F508del-CFTR)的成熟,从而纠正囊性纤维症中常见的CFTR突变,在fisher大鼠甲状腺细胞中EC50为0.1 μM。
了解更多
- Kusumika Saha, .et al. Pharmacological chaperone-rescued cystic fibrosis CFTR-F508del mutant overcomes PRAF2-gated access to endoplasmic reticulum exit sites, Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
- Heledd H Jarosz-Griffiths, .et al. Different CFTR Modulator Combinations Downregulate Inflammation Differently in Cystic Fibrosis, Elife, 2020, Mar 2;9:e54556 PMID: 32118580
- 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
- Junko Kido, .et al. Cystic Fibrosis Transmembrane Conductance Regulator Reduces Microtubule-Dependent Campylobacter jejuni Invasion, Infect Immun, 2017, Oct; 85(10): e00311-17 PMID: 28784926
-
CFTR corrector
VX-661是另一种正在开发中的用于治疗囊性纤维化的囊性纤维化跨膜电导调节器(CFTR)校正器。
了解更多
- Kusumika Saha, .et al. Pharmacological chaperone-rescued cystic fibrosis CFTR-F508del mutant overcomes PRAF2-gated access to endoplasmic reticulum exit sites, Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
-
K+ channel and CFTR Cl- channel blocker
Glyburide (Glibenclamide) 是一种抗糖尿病化合物,是一类磺脲类药物。
了解更多
-
-
CFTR 抑制剂
CFTR inhibitor II,也称为GlyH-101,是一种甘氨酸酰肼,可选择性和可逆地阻断CFTR通道(Ki = 4.3 uM)。
了解更多
- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
-
CFTR chloride channel 抑制剂
PPQ-102是一种化合物,其靶向cftr的胞内核苷酸结合结构域,并以电压依赖性和可逆的方式抑制cftr介导的氯离子电流。
了解更多
-
Protein translocation 抑制剂
Brefeldin A阻断ADP-核糖基化因子与高尔基体的结合并抑制GDP-GTP交换。
了解更多
-
ATPase 拮抗剂
PF 3716556是H+,K+-ATPase酶抑制剂(在人类重组离子渗漏试验中PIC50 = 6)。
了解更多
-
protein tyrosine phosphatases inhibitor
Sodium orthovanadate是化合物Na3VO4。 它是蛋白质酪氨酸磷酸酶,碱性磷酸酶和许多ATPase的抑制剂,很可能充当磷酸盐类似物。
了解更多
-
Artemisinin及其衍生物是一类药物,在所有当前针对恶性疟原虫疟疾的药物中具有最快的作用。
了解更多
-
Ciclopirox是一种合成的抗真菌药物。它可以抑制酵母糠醛马拉丝霉的生长,并通过中断Na+K+ ATPase来抑制膜转移系统,从而发挥作用。
了解更多
- Katsuhisa Morita, .et al. Decomposition profile data analysis of multiple drug effects identifies endoplasmic reticulum stress-inducing ability as an unrecognized factor, Sci Rep, 2020, 10: 13139 PMID: 32753643