act 1

ACT 178882 is a new Renin inhibitor (IC50: 1.4 nM).

Ponesimod (ACT-128800) 是一种选择性 S1P1可口服激动剂，在放射性配体结合试验中的 IC50值为 6 nM。它可高效激活 S1P1介导的信号转导，EC50为5.7 nM。它可预防淋巴细胞介导的组织炎症，具有潜在的免疫调节活性。

ACT-1016-0707 (Compound 49)是一种口服活性及选择性的LPA1受体拮抗剂，主要用于纤维化疾病的研究领域。

ACT-1004-1239 是一种可口服且具有选择性和高效性的 CXCR7 拮抗剂，具有免疫调节和髓鞘促生作用，用于研究炎性脱髓鞘疾病。

Setipiprant (ACT-129968) 是一种口服的选择性 CRTH2 拮抗剂，IC50为6.0 nM。

3-MATIDA 是一种有效的 mGluR-1 拮抗剂（IC50：6.3 μM，大鼠 mGluR-1a）。显示出 ≥ 40 倍于其他受体的选择性：mGluR-5、mGluR-2、mGluR-4 (mGluR-4a) (IC50 > 300 μM)、NMDA 和 GluR (AMPA) (IC50 = 250 μM)。 3-MATIDA 在体外培养的鼠皮质细胞和大鼠海马切片培养物中充当神经保护剂。

Triamterene 是压敏型上皮钠离子通道 （ENaC） 阻断剂，有利尿作用，还可以作为 TGR5 受体的抑制剂，对 TGR5 激活诱导的 GLP-1 分泌和 cAMP 水平升高均呈剂量依赖性降低。

1-Aminocyclobutanecarboxylic acid (ACBC) 是一种NMDA 受体部分激动剂，作用于 NR1 甘氨酸位点。

Berberine (Umbellatine) 属于生物碱类天然产物，可以激活 AMPK、抑制 DNA 拓扑异构酶、诱导 ROS 生成。Berberine 具有抗肿瘤、抗菌、降血糖、降血脂等生物学活性。

Ginsenoside Rg2 (Chikusetsusaponin I) 是一种人参的主要活性成分。它能够降低Aβ1-42积聚，抑制脂多糖介导的VCAM-1和ICAM-1表达的增加。

Diacylglycerols (DAG) are generated through the hydrolysis of membrane phospholipids and function as lipid second messengers by activating protein kinase C (PKC) and modulating cell growth and apoptosis. Additionally, they act as precursors for DAG kinases in the synthesis of phosphatidic acid, a crucial lipid messenger. The compound 1-NBD-decanoyl-2-decanoyl-sn-glycerol incorporates a nitrobenzoxadiazole (NBD) fluorophore at the ω-end of its terminal decanoyl chain, using the structure of 1,2-didecanoyl-sn-glycerol as a model for diacylglycerol. This molecule is expected to exhibit excitation and emission peaks at roughly 470/541 nm, paralleling those of various NBD-labeled phospholipids. Fluorescently labeled lipids, such as this, are instrumental in exploring their interactions with proteins, their uptake by cells and liposomes, and in developing assays for lipid metabolism research.

Prostaglandin F1α (PGF1α) is the putative metabolite of dihomo-γ-linolenic acid (DGLA) via the cyclooxygenase (COX) pathway. Both PGF1α and PGF2α have been shown to act as priming pheromones for male Atlantic salmon with a threshold concentration of 10-11 M. [1] PGF1α binds to the ovine corpus luteum FP receptor at only 8% of the relative potency of PGF2α. [2] It is only half as active as PGF2α in inducing human respiratory smooth muscle contractions in vitro. [3]

Momordin Ic (Momordin 1c) 是山茱萸的主要皂苷成分，通过氧化应激调控线粒体功能障碍诱导细胞凋亡，具有抗癌活性。

TGR5 Receptor Agonist 3 是一种 G 蛋白偶联胆汁酸受体 1（GPBAR1，TGR5）激动剂软药化合物，能够降低胆囊充盈，表现出良好的胆囊安全性，能够作用于 hTGR5 (EC50: 16.4 nM) 和 mTGR5 (EC50: 209 nM)。

Enpp-1-IN-13 是外核苷酸焦磷酸酶 磷酸二酯酶（ENPP）抑制剂，能够作用于 ENPP1 (IC50: 1.29 μM) 和 ENPP3 (IC50: 20.2 μM)，表现出抗癌作用。

GPVI antagonist 2 (Compound 1) 是一种潜在的 Glycoprotein VI (GPVI) 拮抗剂，能够作用于胶原蛋白 (IC50: 0.35 μM)、CRP (IC50: 0.80 μM)、convulxin (IC50: 195.2 μM)、凝血酶 (IC50: 81.38 μM)。其中糖蛋白 VI (GPVI) 是一种血小板主要胶原受体，是有效的、安全的抗血栓研究靶点。GPVI antagonist 2 是一种很有前途的抗血小板药物。

hCA XII II IX-IN-1 是人碳酸酐酶 (hCA) 的有效抑制剂，能够作用于 hCA I (IC50: 2.6 μM)、 hCA II (IC50: 0.004 μM)、hCA IX (IC50: 0.005 μM) 和 hCA XII (IC50: 0.001 μM)。hCA XII II IX-IN-1 表现出抗癌效果。

Ambuphylline (Bufylline) 是茶碱的衍生物，可能通过抑制磷酸二酯酶发挥作用。Ambuphylline 是一种支气管扩张剂，可用于哮喘和其他肺部疾病的研究。

ACT-462206 是一种可口服且可穿过血脑屏障的Orexin 1 Orexin 2 受体拮抗剂。ACT-462206 具有高效性，可用于研究睡眠和焦虑。

Globotetraosylceramides are bioactive neutral glycosphingolipids. They are the major glycolipids in human erythrocytes. They act as receptors for the Shiga toxins Stx1, Stx2, and Stx2e, the cytotoxic protein pierisin-1, and parvovirus B19. Globotetraosylceramides increase the expression of proteins responsible for enamel deposition, including ameloblastin, amelogenin, and enamelin, in dental epithelial cells and activate the ERK and p38 MAPK signaling pathways. Levels of globotetraosylceramides are elevated in fibroblasts from patients with salt and pepper syndrome, a neurocutaneous condition characterized by intellectual disability and hyper- and hypo-pigmented skin. Globotetraosylceramides (porcine RBC) contains a mixture of globotetraosylceramides with variable fatty acyl chain lengths isolated from porcine red blood cells.

E3 ligase Ligand 10 serves as a ligand for E3 ubiquitin ligase and can be conjugated to a protein ligand through a linker, resulting in the formation of PROTACs. These PROTACs act as inducers of ubiquitination-mediated degradation, specifically targeting cancer-promoting proteins[1].

Phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) act synergistically in promoting cancer. Wortmannin is a potent inhibitor of PI3K enzymes, while rapamycin blocks mTOR Complex 1 TORC1. Wortmannin-rapamycin conjugate consists of analogs of 17-hydroxy wortmannin and rapamycin conjugated via a prodrug linker. Hydrolysis of the prodrug linker in vivo releases the inhibitors. The wortmannin-rapamycin conjugate inhibits the growth of HT-29 colon tumors and A498 renal tumors in mice better than rapamycin alone. Also, the conjugate, when given in combination with the VEGF-blocker bevacizumab, produces substantial regression of larger A498 tumors. Finally, the wortmannin-rapamycin conjugate is tolerated better than an equivalent mixture of the inhibitors.

Annonacin is an Acetogenin and promotes cytotoxicity via a pathway inhibiting the mitochondrial complex and it is the active agent found in Graviola leaf extract to act as an inhibitor of sodium potassium (NKA) and sarcoplasmic reticulum (SERCA) ATPase pu

ACT-678689 (Compound Example 1.53.4) 是一种色氨酸羟化酶 (TPH) 抑制剂，IC50=8 nM。