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.

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.

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).

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。

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。

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。

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。

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。

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。

ARN25499 (compound 15) 是一类CDC42抑制剂，适用于开展癌症研究。

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].