arn

Sacubitril/Valsartan (LCZ696) is an orally bioavailable, dual angiotensin II receptor and neprilysin inhibitor for the treatment of hypertension and heart failure.

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 inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) activity, with an IC50 of approximately 34 μM[1].

ARN 077 enantiomer (19) is the less active isomer of ARN 077, with an IC50 value of 3.53 μM against rat NAAA.

ARN14974 is a benzoxazolone carboxamide. ARN14974 is a potent inhibitor of acid ceramidase with IC50 of 79 nM[1].

ARN-6039, an orally available inverse agonist of RORγ, targets Autoimmune Neuroinflammatory Demyelinating Disease. Its efficacy was demonstrated in a RORγ-activated IL-17A Prom/LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 release from CD4+T cell assays (220 nM).

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 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. It inhibits DNA relaxation with an IC50 of 2 μM, compared to 120 μM for Etoposide. ARN-21934 exhibits favorable in vivo pharmacokinetic properties and shows promise in anticancer research, displaying affinity for topoIIα with an IC50 of 2 μM and for topoIIβ with an IC50 of 120 μM. It demonstrates activity against human cancer cell lines including melanoma (A375: 12.6 μM, G-361: 8.1 μM), breast (MCF7: 15.8 μM), endometrial (HeLa: 38.2 μM), lung (A549: 17.1 μM), and prostate (DU145: 11.5 μM) cancer cells. Following a single intraperitoneal injection of 10 mg/kg, ARN-21934 achieves a peak plasma concentration of 0.68 μg/mL in 15 minutes, with a half-life of 149 minutes, and remains detectable in plasma and the brain for up to 360 minutes. [1] Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.

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 is a FAAH-like anandamide transporter (FLAT) inhibitor (IC50: 1.8 μM).

ARN-3236 is an orally active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50 values of <1 nM for SIK2, 21.63 nM for SIK1, and 6.63 nM for SIK3. ARN-3236 exhibits anti-cancer activity.

ARN23746 (IAMA-6) is a selective NKCC1 inhibitor with neuroprotective activity, used in the research of brain diseases including drug-resistant epilepsy (such as temporal lobe epilepsy TLE, Dravet syndrome DrS), autism spectrum disorder ASD, and Down syndrome DoS.

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 is an inhibitor of amyloid precursor protein (APP)and amyloid-β (Aβ) secretion.

ARN 11391 enhances the function of the IP3-gated calcium channel ITPR1 (Inositol 1,4,5-trisphosphate (IP3) receptor type 1), boosting intracellular calcium ion signaling by directly targeting ITPR1. Furthermore, ARN 11391 amplifies calcium signaling in cells with mutant ITPR1 linked to SCA29, a variant of spinocerebellar ataxia.

ARN22089 is an oral active CDC42 GTPase interaction inhibitor that blocks tumour growth in BRAF mutant mouse melanoma models and patient-derived xenografts (PDXs) in vivo.

ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA, exhibiting a broad analgesic profile [1] [2].

ARN25068 is a potent inhibitor of GSK-3β, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].

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 is an F508del-CFTR corrector with an EC50 of 38 pM in human bronchial epithelial cells. It enhances the maturation and function of F508del-CFTR at the cell membrane, influencing ion transport and secretion, thereby addressing the pathological mechanisms of cystic fibrosis (CF).

ARN25499 (compound 15) is an inhibitor of CDC42. It is applicable for research related to cancer.

ARN21929 is a topoisomerase II (TopoisomeraseII) inhibitor with an IC50 of 4.5 μM. It exhibits favorable kinetic and thermodynamic solubility and metabolic stability. However, ARN21929 shows poor antiproliferative activity against A549, DU145, MCF7, HeLa, and A375 cells. It is useful for tumor research.