ca2+flux

CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively.

Senicapoc (ICA-17043) 是有效的，选择性的Gardos 通道 (Ca2+激活的 K+通道;KCa3.1) 阻断剂，IC50为 11 nM。Senicapoc 阻断人红细胞的 Ca2+诱导的铷通量，IC50为 11 nM， 抑制红细胞脱水的IC50为 30 nM。

MCHR1 antagonist 2 是有效的黑色素聚集激素受体 1 拮抗剂，IC50为 65 nM。它也抑制hERG，在IMR-32 细胞中的IC50为 4.0 nM。

ML218 hydrochloride is a selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor (Cav3.2 and Cav3.3 with IC50s of 310 nM and 270 nM , respectively).

ML218 是一种具有口服活性、选择性、高效性且可穿透血脑屏障的 T 型 Ca2+ 通道抑制剂（Cav3.2 和 Cav3.3 的 IC50 分别为 310 nM 和 270 nM）。ML218 可抑制丘脑下核（STN）神经元的突发性活动。

AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected t

AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator and it has an IC50 of 1.2 nM for CCR2 Ca2+ flux [1][2][3].

CCR1 antagonist 8, a third azaindazole series compound, is a CCR1 antagonist (IC50: 1.8 nM in Ca2+ flux assay).

Bryonolic acid (20-epi-Bryonolic acid) 是一种从 Sandoricum indicum 提取的三萜类化合物，具有免疫调节、抗炎，抗氧化和抗癌等活性，通过抑制Ca2+内流和调节Ca2+-CaMKII-CREB信号通路中的基因表达来避免PC12细胞免受NMDA诱导的细胞凋亡反应。

Linoleic Acid Amide (Linoleamide) 衍生自亚油酸，通过抑制肌肉 内质网 Ca2+-ATP 酶来调节 Ca2+ 通量。

Emetine hydrochloride (NSC 33669)，一种从ipecac根部提取的生物碱，用于临床上作为催吐及抗原生动物药物。它能够降低HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α)、PDK1、RhoA、Rho-kinases (ROCK1 and ROCK2)和BRD4，抑制细胞自噬，并展现抗疟疾、抗病毒、抗细菌及抗变形虫效果。

This novel compound is an orally bioavailable antagonist of P2X3 P2X2 3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2 3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2 3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1 2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes.

Gypenoside L 是存在于绞股蓝中的一种皂苷，可增加 SA-β-半乳糖苷酶活性，促进衰老相关分泌细胞因子的产生。它还可以激活p38和ERK MAPK 通路和NF-κB 通路以诱导衰老，具有抗肿瘤和抗炎活性。