arn

Sacubitril Valsartan (LCZ696)，以1:1摩尔比由Valsartan（一种ARB）和Sacubitril（AHU377）组成，为创新口服血管紧张素受体-脑啡肽酶（ARN）双重抑制剂，旨在治疗高血压与心力衰竭。其作用机制包括抑制炎症、氧化应激及细胞凋亡，有助于改善糖尿病心肌病。

ARN 077 is a selective N-acylethanolamine acid amidase (NAAA) inhibitor (IC50: 7 nM for human NAAA). ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS.

ARN-3236 是一种口服有活性的、具有选择性的盐诱导激酶2 (SIK2)抑制剂，它能够抑制SIK1 (IC50:21.63 nM)、SIK2(IC50<1 nM)和 SIK3(IC50:6.63 nM)。它具有抗肿瘤作用。

ARN19702 是一种选择性，具有口服活性的，可逆的，可透过血脑屏障的 N-乙酰乙醇胺酸酰胺酶 (NAAA) 抑制剂，对人 NAAA 的 IC50为 230 nM。ARN19702 具有广泛的镇痛作用。

ARN19874 is a selective, reversible uncompetitive N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) activity inhibitor. With an IC50 of ~34 μM[1].

ARN14974 是一种有效的全身活性的胞内酸性神经酰胺酶抑制剂 (IC50=79 nM)，是一种苯并恶唑酮甲酰胺化合物。

ARN-6039 is an orally available inverse agonist of RORγ for Autoimmune Neuroinflammatory Demyelinating Disease. The activity of ARN-6039 against RORγ was demonstrated in a RORγ-activated IL-17A Prom LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 r

ARN14686 is an activity-based affinity probe for the detection of N-acylethanolamine acid amidase (NAAA) using click chemistry.

ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂，具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM，ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。

ARN24139 is a topoisomerase II poison (IC50= 7.3 μM in a topoisomerase II decatenation assay).1It inhibits proliferation of DU145, HeLa, and A549 cells (IC50s = 4.7, 3.8, and 3.1 μM, respectively). 1.Arencibia, J.M., Brindani, N., Franco-Ulloa, S., et al.Design, synthesis, dynamic docking, biochemical characterization, and in vivo pharmacokinetics studies of novel topoisomerase II poisons with promising antiproliferative activityJ. Med. Chem.63(7)3508-3521(2020)

ARN19689 is an effective inhibitor of human NAAA, demonstrating high potency in the low nanomolar range (IC 50 = 0.042 μM). The compound acts through a non-covalent mechanism, highlighting its ability to interact with the enzyme for inhibition.

ARN272 是大麻素转运抑制剂的一种。

ARN23746 is a NKCC1 Inhibitor for the Treatment of Core Symptoms in Down Syndrome.

ARN 14494 is a potent serine palmitoyltransferase inhibitor (SPT; IC50 = 27.3 nM). ARN 14494 inhibits synthesis of long chain ceramides and dihydroceramides in an in vitro model of Alzheimer's diease. The compound prevents the synthesis of proinflammatory cytokines and the oxidative stress-related enzymes iNOS and COX-2 in mouse primary cortical astrocytes. ARN 14494 is neuroprotective against β-amyloid 1-42 induced neurotoxicity in primary cortical neurons co-cultured with astrocytes.

ARN2966 是高效的，针对 APP 表达的转录后调节剂，能够抑制 APP 的表达从而使 Aβ的量降低。

ARN 11391是ITPR1 (Inositol 1,4,5-trisphosphate (IP3) receptor type 1)的增效剂，它直接作用于ITPR1，从而增强细胞内钙离子信号。ARN 11391还能增强表达突变型ITPR1细胞中的钙信号，这与SCA29型脊髓小脑共济失调有关。

ARN22089是一种CDC42 GTPase相互作用抑制剂，具有口服活性，能够在体内阻断BRAF突变小鼠黑色素瘤模型和患者来源的异种移植物（PDXs）的肿瘤生长。

ARN25068是三种蛋白激酶(GSK-3β、FYN和DYRK1A)的亚微摩尔抑制剂，可用于治疗tau相关神经系统疾病。

ARN14988 is a potent inhibitor of acid ceramidase (IC50 = 12.8 nM for the human enzyme). It inhibits acid ceramidase activity and increases levels of C16 dihydro ceramide and C16 ceramide in A375, G361, M14, MeWo, MNT-1, and SK-MEL-28 melanoma cells. ARN14988 also reduces growth of A375 and G361 melanoma cells (EC50s = 41.8 and 67.7 μM, respectively).

ARN16186; ARN 16186; ARN-16186 is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. This compound targets and inhibits the PI3K enzyme, which may result in the inhibition of the PI3K Akt signaling pathway and thus inhibit cell growth and induce apoptosis in susceptible tumor cell populations.

ARN23765 是一种 F508del-CFTR 校正剂，在人支气管上皮细胞中的EC50为 38 pM。它能够改善细胞膜中 F508del-CFTR 的成熟和功能，影响离子的运输与分泌，从而纠正囊性纤维化 (CF) 的病理机制。

ARN726 是 N-酰基乙醇胺酸酰胺酶的有效抑制剂 (IC50 = 0.073 μM)，它以剂量依赖性方式降低饮酒动机。

ARN1468 (compound 5) is a highly effective orally active inhibitor of serpins. Inhibition of serpins activity by ARN1468 enables release of proteases, thereby reducing prion accumulation. ARN1468 demonstrates pronounced anti-prion effects in ScGT1 RML, ScGT1 22L, ScN2a RML, and ScN2a 22L cell lines, with EC 50 values of 8.64, 19.3, 11.2, and 6.27 μM [1].

ARN5187 是一种亲溶酶体化合物，是 REV-ERBβ的配体。ARN5187抑制 REV-ERB 介导的转录调控和细胞自噬。ARN5187 显示出溶酶体效力和细胞毒性，可诱导细胞凋亡 (apoptosis)。