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Sinbaglustat (OGT2378) (OGT2378) 是葡萄糖神经酰胺合成酶 (GCS) 和非溶酶体葡萄糖神经酰胺酶 (GBA2) 的双重抑制剂。Sinbaglustat 是一种可透过血脑屏障的的口服N-烷基亚氨基糖。Sinbaglustat 可用于治疗溶酶体贮积症和研究溶酶体功能障碍相关的中枢神经退行性疾病。

Macitentan (ACT-064992) 是一种内皮素受体拮抗剂，用于治疗肺动脉高压。

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-389949 是一种高效的甲酰肽受体 2 脂蛋白 A4 受体(FPR2) (ALX)选择性激动剂，对 FPR2 ALX 进行内化入单核细胞的EC50值为 3 nM。它对炎性疾病具有潜在的研究价值。

Apinocaltamide(ACT-709478)是一种可口服和选择性的T型Ca 2+ 通道 (T-type calcium channel) 阻滞剂，具有可透过血脑屏障（BBB）的特性，对Cav3.1, Cav3.2和 Cav3.3的IC50=6.4~18nM，常用于癫痫的研究。

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

ACT-451840能够消除敏感和耐药的恶性疟原虫株，具有口服活性、强效、低毒性的优点，在疟原虫的所有无性血液阶段起效迅速，作用机制类似于青蒿素衍生物。在体内实验中，ACT-451840在30 mg kg剂量下表现出极好的抗疟效果，寄生虫减少率达到99.80%。

ACT-335827 是一种可口服的、脑渗透性 orexin 1 型 (orexin type 1) 受体选择性拮抗剂。ACT-33582 作用于 OXR1 和 OXR2 的 IC50值分别是 6 nM 和 417 nM。ACT-33582 可用于神经系统疾病的相关研究。

ACT-451840 is a drug of antimalarial activity. It has effective activity against sensitive and resistant Plasmodium falciparum strains.

ACT-209905 is an agonist of S1P1 receptor.

ACT-387042 is a Bacterial Topoisomerase Inhibitor, it has broad-spectrum activity against Gram-positive and Gram-negative bacteria.

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。

Selexipag (ACT-293987) 是前列环素受体激动剂，可引起肺血管舒张，用于治疗肺动脉高压。

Lucerastat（NBDGJ，芦舍司他）是一种口服的葡萄糖神经酰胺合酶（Glucosylceramide Synthase, GCS）的抑制剂，具有治疗法布里病的潜力。 ​GCS是鞘糖脂合成的关键酶，抑制其活性可减少有害底物的积累。

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

ACT-373898 is a metabolite of the endothelin (ET) receptor type A (ETA) and ETBdual antagonist macitentan .1 1.Dingemanse, J., Sidharta, P.N., Maddrey, W.C., et al.Efficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertensionExpert Opin. Drug Saf.13(3)391-405(2013)

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。

ACT-660602 是口服具有活力的趋化因子受体 CXCR3 拮抗剂 (IC50: 204 nM)。ACT-660602 能够抑制 T 细胞迁移，并在体内急性肺损伤模型中显示出显著作用。ACT-660602 能够用于研究自身免疫性疾病。

Gallamine is an allosteric antagonist at muscarinic M2 acetylcholine receptors and an inhibitor of acetylcholinesterase.

ACT-280778 is a potent L T calcium channel blocker.

SLR080811 is a SphK inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.

ACT-672125 is a Potent CXCR3 Antagonist with Therapeutic Potential in Autoimmune Diseases. ACT-672125 showed good physicochemical properties and safety profile. In a proof-of-mechanism model of lung inflammation, ACT-672125 inhibited the recruitment of CXCR3 expressing T cells into the inflamed lung in a dose-dependent manner.

CHS-828 nicotinate is a CHS-828 salt with Nicotinic acid.. CHS-828 also known as GMX-1778, is a potent and selective NAMPT inhibitor. CHS-828 inhibits cellular synthesis of NAD. CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome. CHS 828 has shown promising anticancer activity in experimental tumor models and primary cultures of cancer cells from patients. CHS 828 showed a synergistic effect with melphalan in 67%, doxorubicin in 47%, etoposide in 38% and Ara-C in 14% of AML samples.

GCC-4401C free base is a factor Xa inhibitor similar to rivaroxaban that is currently under development for venous thromboembolic disease (VTE).