[Ca2 ]i

SMARCA2-IN-2 (Compound I-25) 作为SMARCA2抑制剂，具有IC50值在101-500 μM范围内，主要应用于癌症相关的研究领域。

SMARCA2-IN-7(compound 12),作为 BRM 和 BRG1 的双重抑制剂(IC50 均小于 0.005),展现了抑制肿瘤增殖的效果.对于缺失 BRG1 的 SKMEL5 肿瘤细胞,该化合物在抑制细胞增殖方面显示出强效,其 AAC50 为 13 nM.此外,在 H1299 细胞中,SMARCA2-IN-7 通过降低 KRT880 的表达,达到抑制细胞增殖的目的,AAC50 值为 42 nM.

SMARCA2-IN-8(Compound 13)是针对SWI SNF染色质重塑复合物中的SMARCA2(Brahma 同源物,BRM)和SMARCA4(Brahma 相关基因1,BRG1)的口服有效抑制剂,其IC50值分别为5 nM和6 nM.此化合物能有效抑制携带SMARCA2突变的癌细胞SKMEL5的增殖,AAC50为5 nM,并能下调依赖SMARCA2的KRT80基因的表达,AAC50为10 nM.在小鼠模型中,SMARCA2-IN-8展现出抗肿瘤活性以及良好的药物代谢动力学属性.

SMARCA2-IN-4(Compound 26)作为一种抑制剂,专门针对SWI SNF染色质重塑复合物中的SMARCA的溴结构域.该化合物对PB1(5)、SMARCA2B及SMARCA4展示出较高的亲和性,Kd 值分别为124 nM、262 nM 和 417 nM.

SMARCA2-IN-1 (Compound I-19),作为SWI SNF染色质重塑复合物SMARCA2的抑制剂,在H1299细胞中展示出IC50值超过1000 nM.

SMARCA2-IN-9(化合物 11)作为一种有效的SMARCA2、PBRM1 溴结构域 2 (PBRM1(2)) 以及PBRM1 溴结构域 5 (PBRM1(5)) 抑制剂,其Kd值显示为1.6 μM、2.5 μM 和 3.95 μM.

Aprikalim (RP 52891) 是一种三磷酸腺苷钾通道（KATP）开启剂，可保护脊髓缺血兔模型中的神经受到损伤。Aprikalim 抑制血管收缩，抑制心肌麻痹期间 [Ca2+]i 升高，可以用于研究心血管疾病。

(-)-Menthol (Levomenthol) 分离自薄荷油，L-Menthol 是瞬时受体电位 M8 (TRPM8)的激活剂，TRPM8 是 Ca2+-可渗透的非选择性阳离子通道，并增加 [Ca2+]i。L-Menthol 具有抗肿瘤活性。

Halofuginone hydrobromid 是Febrifugine 的衍生物，是竞争性脯氨酰-tRNA 合成酶抑制剂。它是 I 型胶原合成的特异性抑制剂，并通过抑制TGF-β活性可减轻骨关节炎。它具有抗疟疾、抗炎、抗癌、抗纤维化作用。

Nebracetam hydrochloride (WEB 1881 FU hydrochloride) 是促智 M1-毒蕈碱的激动剂。 它诱导细胞内 Ca2+ 浓度升高， EC50 为 1.59 mM。

CALP3 acetate(261969-05-5 free base) 是一种有效的 Ca2+ 通道阻滞剂，可激活 Ca2+ 结合蛋白的 EF 手基序。 它可以通过调节钙调蛋白 (CaM)、Ca2+ 通道和泵的活性在功能上模拟增加的 [Ca2+]i。

18:0 LYSO-PE是一种诱导[Ca2+]i增加的化合物，18:0 LYSO-PE可用作电喷雾质谱（ESI-MS） MS进行脂质分析的磷脂（PL）标准。

L-365260 是一种可口服且具有选择性和高效性的非肽胃泌素和脑胆囊收缩素受体 (CCK-B) 拮抗剂。L-365260 抑制 CCK-8S 诱导的 [Ca2+]i 增加，可阻断应激引起的内脏超敏反应，可阻断 CCK-4 的抗探索作用，可用于研究神经系统Ojibwa和内分泌疾病。

o-3M3FBS 是 m-3M3FBS 的阴性对照。它以独立于 PLC 的机制及拮抗方式抑制内向和外向电流。它以与 m-3M3FBS 竞争的方式增加 [Ca2+]i 增加。

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).

Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. Nebentan inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors in a concentration dependent manner,Ki values are 0.697 nM and 1.53 nM for human and rat endothelin ETA receptors, respectively. In contrast, YM598 exhibits low affinities for human and rat endothelin ETB receptors, with Ki values of 569 nM and 155 nM,respectively[1].In measurement of intracellular Ca2+ concentration, Nebentan concentration-dependently inhibits the increase in [Ca2+]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC50 values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively[1]. Nebentan (oral administration; 0.1-1 mg kg; 4 weeks) significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy[2].Nebentan (oral administration; 1 mg kg; 30 weeks) significantly ameliorates the poor survival rate of CHF rats, it markedly reduces the hypertrophy of both ventricles as well as pulmonary congestion[2]. [1]. Hironori Yuyama, et al. Pharmacological Characterization of YM598, an Orally Active and Highly Potent Selective Endothelin ET(A) Receptor Antagonist. Eur J Pharmacol. 2003 Sep 30;478(1):61-71. [2]. Akira Fujimori, et al. YM598, an Orally Active ET(A) Receptor Antagonist, Ameliorates the Progression of Cardiopulmonary Changes and Both-Side Heart Failure in Rats With Cor Pulmonale and Myocardial Infarction. J Cardiovasc Pharmacol. 2004 Nov;44 Suppl 1:S354-7.

TAT-Gap19(I130A) is a control peptide for TAT-Gap19, a Cx43 hemichannel blocker. TAT-Gap19(I130A) consists of TAT-GAP19 with a I130A amino acid residue change at a key residue for GAP19 activity. In C6 glioma cells expression Cx43, TAT-GAP19(1130A) does not inhibit [Ca2+]i-triggered ATP release at 200 μM. TAT-Gap19(I130A) is cell permeable.

Rhodojaponin III 是二萜类化合物，提取于Rhododendron molle 叶子，具有抗炎作用。

Barlerin (8-O-Acetylshanzhiside methyl ester) 是一种环孢菌素葡萄糖苷，从中国西藏民间药用植物中分离得到，能够抑制NF-κB 活性。

Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) 是一种长效的、非选择性的钙离子通道 (Ca+channel) 拮抗剂。Bepridil hydrochloride hydrate 是一种钠离子、钾离子通道 (Na+,K+channel) 抑制剂，也是心脏 Na+ Ca2+交换 (NCX1) 抑制剂。Bepridil hydrochloride hydrate 具有抗心绞痛和抗 I 型心律失常作用，能够用于研究心血管疾病。

AL-38022A is a novel synthetic serotonergic (5-HT) ligand that exhibited high affinity for each of the 5-HT2 receptor subtypes (Kicantly lower (>100-fold less) affinity for other 5-HT receptors. In addition, AL-38022A displayed a very low affinity for a broad array of other receptors, neurotransmitter transport sites, ion channels, and second messenger elements, making it a relatively selective agent. AL-38022A potently stimulated functional responses via native and cloned rat (EC50 range: 1.9-22.5 nM) and human (EC50 range: 0.5-2.2 nM) 5-HT2 receptor subtypes including [Ca2+]i mobilization and tissue contractions with apparently similar potencies and intrinsic activities and was a full agonist at all 5-HT2 receptor subtypes.

AL-34662 is a serotonin-2 receptor agonist with antihypertensive action. AL-34662 has a high-affinity for the 5-HT2 receptor and may potentially lead mobilization of [Ca2+]i in h-CM and h-TM cells leading to a decrease in ocular pressure.

Praeruptorin C 是白花前胡中的一种主要成分，是钙拮抗剂，pD2′值为 5.7。

Soyacerebroside II exhibits ionophoretic activity for Ca2+ ion. Soyacerebrosides I and II have modulating the cellular immune response effects, they show obvious inhibitory activity on IL-18 secretion in human peripheral blood mononuclear cells (PBMC).