calcium-activated

DAMGO TFA (78123-71-4(Free base)) 是Mu-opioid 受体的强效选择性激动剂。它也是镇痛药。它刺激钙激活的腺苷酸环化酶相关 cAMP 的产生。通过 TGF-beta1 表达趋化因子和趋化因子受体。增加老鼠的食物摄入量。

Flufenamic acid (Arlef) 是一种非甾体类抗炎剂，是一种邻氨基苯甲酸衍生物，具有镇痛、抗炎和解热的特性。 它用于肌肉骨骼和关节疾病。

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) 是从丹参中提取的丹参酮IIA 的水溶性衍生物，是SOCE 抑制剂，用于心血管疾病的研究。

Ethosuximide (Zarontin) 是一种抗癫痫药物，可改善多种神经退行性疾病模型的表型，且阻断低电压激活的 T 型钙通道。

Tetrandrine (Sinomenine A) 属于天然产物，是一种双苯基异喹啉生物碱，一种钙离子通道抑制剂。Tetrandrine 可抑制电压门控钙离子通道 (ICa) 和 Ca2+ 激活的钾离子通道。

Synta66 是一种钙池操纵钙离子通道 Orai 抑制剂，用于神经系统疾病的研究。

N-(p-amylcinnamoyl) Anthranilic Acid (ACA) 是一种广谱磷脂酶 A2(PLA2) 抑制剂，也是TRP channel 的阻滞剂。ACA 也可逆的抑制钙离子激活氯通道 (calcium-activated chloride channels) ，在心律失常方面具有研究的潜力。

Dihydrocapsaicin (CCRIS1589) 是一种天然来源的辣椒素，是TRPV1的选择性激动剂，同时可以增加 p-Akt 水平。它可以增强低温诱导的神经保护。

T16Ainh-A01 是氨基苯基噻唑，是有效的跨膜蛋白 16A 的抑制剂，抑制 TMEM16A 介导的氯离子电流，IC50约为1 µM。TMEM16A (ANO1)起钙激活氯离子通道(CaCC)的作用。

SKF-96365 hydrochloride (SKF96365) 是store-operated Ca2+entry 抑制剂，也是TRP channel 阻滞剂。它显著抑制豚鼠离体心脏 hERG、hKCNQ1 hKCNE1、hKir2.1 和 hKv4.3 电流，延长QTc 间期。它通过诱导结直肠癌细胞的细胞周期阻滞和凋亡起抗肿瘤作用。

Rimtuzalcap (CAD-1883) 是首创的，选择性的小电导钙激活钾通道 (SK 通道) 正变构调节剂。Rimtuzalcap 可用于运动障碍的研究，包括脊髓小脑性共济失调 (SCA)和特发性震颤 (ET)。

RO2959 Hydrochloride (RO2959 HCl) 是选择性CRAC 通道抑制剂，IC50为 402 nM。它是人IL-2产生的有效抑制剂，有效阻断 T 细胞受体触发的基因表达和 T 细胞功能途径。它是由Orai1 Stim1通道介导的钙存储进入的有效阻滞剂，IC50为 25 nM。

GSK-7975A 是具有口服活性的高效CRAC 通道抑制剂。

CRAC intermediate 1是用于CRAC离子通道系列化合物合成的关键中间体，详细信息来自专利WO 2010122089。

LY255283 是白三烯 B4 (LTB4) 受体的特异性拮抗剂，抑制人外周血多形核白细胞和由钙离子载体 A23187 激活的单核细胞中 LTB(4) 的产生。

Gomisin J 是在五味子中发现的小分子量木脂素，具有血管舒张活性，在非酒精性脂肪性肝病方面有研究潜力。 它通过激活 AMPK、LKB1 和 Ca2+ 钙调蛋白依赖性蛋白激酶 II 以及抑制 HepG2 细胞中的胎球蛋白 A 来调节脂肪生成酶和脂肪分解酶以及炎症分子的表达，从而抑制脂质积累。

Flindokalner (BMS-204352) 是一种钾离子通道调节剂。它是大电导钙激活 K 通道正向调节剂。它是在 HEK293 细胞中表达的所有神经元 Kv7通道亚型的正调节剂。它在 Kv7.1 通道 (Ki=3.7 μM) 处显示负调节活性，并充当 GABAA 受体的负调节剂。它在体内显示出抗焦虑功效。

BMS-191011 (BMS-A) 是一种大电导 Ca2+激活的钾通道 (Ca2+-activated potassium (maxi-K) channel) 激活剂，在中风模型中有研究价值。

CRAC intermediate 2是CRAC 抑制剂合成的中间体化合物。

SB297006 是一种CCR3拮抗剂，IC50为39 nM。它能够显著抑制 CCL11 处理的神经祖细胞的增殖和神经球形成。

TRPM4-IN-1 (4-chloro-2-(2-(2-chlorophenoxy)acetamido)benzoic acid) 是一种有效的阳离子通道TRPM4选择性抑制剂，IC50为 1.5 μM。TRPM4-IN-1 在心脏病和前列腺癌中具有研究价值。

YM-58483 (BTP2) 是一种特异性有效的 CRAC 通道和随后的 Ca2+ 信号抑制剂，可阻断钙池操纵的阳离子内流 (SOCE)。

Benzthiazide (Lemazide) 是长效利尿剂及抗高血压剂。它也是碳酸酐酶 9 的抑制剂，他对 CA9，CA2 和 CA1 的 Ki 分别为 8.0，8.8 和 10 nM。它对肿瘤细胞增殖具有抑制作用。

SKA-111 是一种选择性钙离子激活的钾离子通道 (potassium phannel ) KCa3.1 激活剂，可引起猪内皮细胞膜超极化。SKA-111结合在CaM N-瓣和S4-S5接头之间的界面中，能够改善 Bradykinin 诱导的离体大鼠心脏的冠状动脉扩张，可用于研究心血管疾病。

Ophiopogonin D 是从麦冬的块茎中分离的一种天然产物，是罕见的天然存在的 C29甾体糖苷。它是一种 CYP2J3 诱导剂，用于炎症和心血管疾病的相关研究。

Talniflumate (Somalgen) 是一种钙激活氯离子通道 (hCLCA1 mCLCA3) 阻滞剂，可减少动物模型和细胞培养中的粘蛋白合成和释放。它通过抑制环氧合酶，并抑制 Cl- HCO3- 交换活性，具有抗炎作用。它还增加了远端肠梗阻综合征囊性纤维化小鼠模型的存活率。

CaCCinh-A01 是钙激活氯离子通道和TMEM16A 抑制剂，IC50值分别为 10 和 2.1 μM。

Zegocractin (CM-4620) 是一种钙离子释放激活通道的抑制剂，对Orai1 STIM1和Orai2 STIM1的IC50值分别为 119 和 895 nM。

(±)-Liquiritigenin ((±)-4',7-Dihydroxyflavanone) 是从 Angelica keiskei 提取得到的类黄酮，抑制钙活化的氯离子通道TMEM16A。(±)-Liquiritigenin 诱导细胞凋亡增加和 Caspase3 活性增强。(±)-Liquiritigenin 可用于研究乳腺癌。

NS13001 (N-(4-Chlorophenyl)-2-(3,5-dimethyl-1H-pyrazol-1-yl)-9-methyl-9H-purin-6-amine) 是口服有效的 SK 通道选择性正向变构调节剂。NS13001 对 SK2 和 SK3 通道的 EC50分别为 1.8 μM 和 0.14 μM。NS13001 在脊髓小脑共济失调 2 型和其他小脑共济失调方面具有研究价值。

5J-4 是一种有效的钙释放激活钙通道 (CRAC) 和钙池操纵性钙内流(SOCE) 阻滞剂。 5J-4 减少 IL-17 的产生并降低 RORα 和 RORγt 的表达。

ChTX-Lq2为Ca2+激活的K+流出抑制剂，Kd值为43 nM。

SOR-C13 is an inhibitor of transient receptor potential cation channel vanilloid family member 6 (TRPV6, CaT1 or CATL) with potential antineoplastic activity. TRPV6 calcium channel inhibitor SOR-C13 binds to TRPV6 and prevents the influx of calcium ions into TRPV6-expressing tumor cells. This inhibits the activation of nuclear factor of activated T-cell (NFAT) transcription complex which may result in an inhibition of calcium-dependent cancer cell proliferation and an induction of apoptosis in tumor cells overexpressing TRPV6.

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol/kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)

Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2是一类具有生物活性的肽，作为蛋白酶激活受体1 (PAR-1) 的选择性激动剂，其特异性优于PAR-2。该肽通过HEK293细胞进行的基于细胞的钙信号传导测定确认了其对PAR-1的高特异性，并可用于研究PAR-1在体内的激活。PAR-1除了介导凝血酶的多种细胞作用外，还与PAR-4协作，参与调控凝血酶诱导的被分类为“凝血型”的肝细胞癌。

Tertiapin 为一种合成蜂毒肽，其结构特征为 Cys3-Cys14 与 Cys5-Cys18 形成的二硫键。此化合物主要作为内向整流钾通道 (potassium Channel) 的阻滞剂，并能抑制钙激活大电导钾通道的活性。Tertiapin (reduced) 常用于研究类风湿性关节炎和多发性硬化症等疾病。（Text revision and optimization for clarity and conciseness, maintaining specific chemical and biomedical terms as requested.）

aliotoxin是神经BK型肽基的抑制剂，对Kv通道和钙激活的钾通道能产生特异性抑制。Kaliotoxin对细胞膜电位和神经元兴奋性的调控具有研究意义。其产品编号为 T37808，CAS号为 145199-73-1

(±)13,14-EDT是一种氧脂和腎上腺酸的代谢产物，通过细胞色素P450（CYP）途径形成。在50 nM的浓度下，它能激活分离的大鼠冠状小动脉平滑肌细胞中的大导电钙激活钾通道（KCa1.1/BK），并导致分离的猪小动脉扩张（EC50 = 12 pM）。(±)13,14-EDT还能使用TP受体激动剂U-46619预收缩的分离牛冠状动脉放松。

1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE is a phospholipid that contains stearic acid at the sn-1 position and 15(S)-HETE at the sn-2 position. It is formed in human peripheral monocytes activated by the calcium ionophore A23187 by direct oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE by 15-LO. Phosphoethanolamine (PE) HETEs (PE-HETEs), including 1-stearoyl-2-15(S)-HETE-sn-glycero-3-PE, are the main source of esterified HETE in ionophore-activated monocytes.

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis[1][2]. Proteinase-activated receptors (PARs) are a family of G protein-coupled receptors activated by the proteolytic cleavage of their N-terminal extracellular domain, exposing a new amino terminal sequence that functions as a tethered ligand to activate the receptors.RWJ56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM) while being quite selective relative to collagen and the thromboxane mimetic U46619 [1].RWJ-56110 dihydrochloride is fully inhibits thrombin-induced RASMC proliferation with an IC50 value of 3.5 μM. RWJ-56110 dihydrochloride shows blockade of thrombin's action with RASMC calcium mobilization (IC50=0.12 μM), as well as with HMVEC (IC50=0.13 μM) and HASMC calcium mobilization (IC50=0.17 μM)[1].RWJ56110 (0.1-10 μM; 24-96 hours) inhibits endothelial cell growth dose-dependently, with half-maximal inhibitory concentration of RWJ56110 is approximately 10 μM[2].RWJ56110 (0.1-10 μM; 6 hours) inhibits DNA synthesis of endothelial cells in a thymidine incorporation assays. Endothelial cells are in fast-growing state (50-60% confluence), RWJ56110 inhibits cell DNA synthesis in a dose-dependent manner, but when cells that are in the quiescent state (100% confluent), the inhibitory effect of PAR-1 antagonists is much less pronounced[2].RWJ56110 (0.1-10 μM; pretreatment for 15 min) inhibits thrombin-induced Erk1 2 activation in a concentration-dependent manner. However, when endothelial cells are stimulated by FBS (final concentration 4%), it reduces partially the activated levels of Erk1 2[2].RWJ56110 (30 μM; 24 hours) has an inhibitory effect on endothelial cell cycle progression. It reduces the percentage of cells in the S phase, while alterations in the percentages of G1 and G2 M cells are less pronounced[2]. Western Blot Analysis[2] Cell Line: Endothelial cells [1]. Andrade-Gordon, et al.Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. oc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62. [2]. Panagiota Zania, et al. Blockade of angiogenesis by small molecule antagonists to protease-activated receptor-1: association with endothelial cell growth suppression and induction of apoptosis. J Pharmacol Exp Ther. 2006 Jul;318(1):246-54.

KCa2 (small conductance Ca2+-activated potassium) channel negative allosteric modulator (IC50 = 1.1 μM). Increases the EC50 of Ca2+ on KCa2.3 channels by ~3-fold. Prolongs atrial effective refractory period (AERP) in rats. Reduces atrial fibrillation (AF) duration and prolongs atrial refractoriness without affecting ventricular refractory period in an animal AF model. Diness et al (2017) Termination of vernakalant-resistant atrial fibrillation by inhibition of small-conductance Ca2+-activated K+ channels in pigs. Circ.Arrhythm.Electrophysiol. 10 e005125 PMID:29018164 |Simó-Vicens et al (2017) A new negative allosteric modulator, AP14145, for the study of small conductance calcium-activated potassium (KCa2) channels. Br.J.Pharmacol. 174 4396 PMID:28925012

Fargesone B inhibits the vascular smooth muscle contraction by suppressing the voltage- and receptor-activated calcium influxes in a nonselective manner.

Potent KV1.3 channel blocker (IC50 = 36 pM). Displays no effect at calcium-activated channels. Reduces VEGF-induced transmembrane calcium influxes and nitric oxide production in human endothelial cells.

VU0531245为SLACK通道抑制剂，其IC50值达2.1 μM。

Mibefradil dihydrochloride hydrate (Ro 40-5967 dihydrochloride hydrate) 是一种长效的钙离子通道拮抗剂。Mibefradil dihydrochloride hydrate 通过对低电压激活 (T) 钙通道的亲和力高于对高电压激活 (L) 钙通道的亲和力来发挥作用。Mibefradil dihydrochloride hydrate 能够降压药。

Noxiustoxin为墨西哥蝎子Centruroides noxius毒液中的一种毒素，它能够抑制电压依赖性钾通道（Kv1.3，IC50=360 nM）及钙激活钾通道。该毒素在神经炎症疾病中具有重要作用。

Calcicludine是Dendroaspis angusticeps产毒蛋白，针对高电压激活的calcium channel（特别是L型）有抑制作用，IC50为88 nM，影响兴奋性突触传递。

5(S),12(S)-DiHETE is a natural bioactive lipid derived from arachidonic acid . It is synthesized by glycogen-induced rabbit peritoneal polymorphonuclear leukocytes (PMNLs) incubated with AA. 5(S),12(S)-DiHETE can be produced by successive oxygenation of AA by 5-lipoxygenase (5-LO) in platelets and 12-LO in leukocytes. It can also be synthesized from 12(S)-HETE by 5-LO, in the presence of 5-LO activating protein (FLAP), activated with calcium ionophore. 5(S),12(S)-DiHETE is an epimer of leukotriene B4 that is weakly chemotactic for PMNL.