Netupitant is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity. Netupitant competitively binds to and blocks the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). SP is found in neurons of vagal afferent fibers innervating the brain-stem nucleus tractus solitarii and the area postrema, which contains the chemoreceptor trigger zone (CTZ), and may be elevated in response to chemotherapy. The NK-receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema. On 10/10 2014 FDA approved netupitant for the treatment of nausea and vomiting in patients undergoing cancer chemotherapy.
Netarsudil, also known as AR-11324, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure.
Nestorone is a steroidal progestin of the 19-norprogesterone group which is used as a hormonal contraceptive in several South American countries. It is a potent progesterone receptor agonist with no androgenic, estrogenic, or glucocorticoid-like activities. It has been used as a female contraceptive and may be useful as a male contraceptive too recently. It does not bind to the estrogen receptor either, but it has some affinity for the glucocorticoid receptor. It appears to act as an agonist, but it does not appear to produce any glucocorticoid side effects unless used at high doses. It has been shown to have neurogenic and neuroprotective activity. It holds back proinflammatory mediators and neuropathology in the wobbler mouse model of motoneuron degeneration. It protected against hippocampus abnormalities and improved functional outcomes of EAE mice, which suggests its potential value. It lacks affinity for the androgen receptor, thus does not produce any androgenic or anabolic effects.
Neratinib, also known as HKI-272 or PB272, is an orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Treatment of cells with this agent results in inhibition of downstream signal transduction events and cell cycle regulatory pathways; arrest at the G1-S (Gap 1/DNA synthesis)-phase transition of the cell division cycle; and ultimately decreased cellular proliferation. Neratinib also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells.
Nepicastat hydrochloride (SYN117, RS-25560-197) is an inhibitor of dopamine beta-hydroxylase that catalyzes the conversion of dopamine to norepinephrine. Nepicastat hydrochloride shows the selective and concentration-dependent inhibition effects on bovine and human dopamine-beta-hydroxylase activity in vitro. In vivo, Nepicastat hydrochloride increases dopamine content and dopamine/noradrenaline ratio in a dose-dependent manner. Nepicastat hydrochloride also produces the similar effects on noradrenaline, dopamine and dopamine/noradrenaline ratio in tissues and plasma of beagle dogs. Nepicastat is currently in Phase II clinical trials in patients with Posttraumatic Stress Disorder.
NEO2734 is an orally active dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM. NEO2734 efficiently reduced the viability of AML cell lines and primary AML cells by inducing apoptosis.
Nelarabine acts by inhibiting DNA synthesis and inducing apoptosis in susceptible cells. Nelarabine demonstrated significant antineoplastic activity with acceptable toxicity.
Neferine is a bis-benzylisoquinoline alkaloid isolated from the green seed embryos Nelumbo Nucifera Gaertn (Lotus) that displays multiple pharmacological activities including anti-tumor, antidepressant-like and antiarrhythmic actions. It potently inhibits proliferation of human osteosarcoma cells while is low-toxic on non-neoplastic human osteoblast cells. It inhibited high glucose-induced endothelial apoptosis via blocking ROS/Akt/NF-κB pathway, which provides the evidence for using Neferine to treat diabetic vasculopathy.
Necrosulfonamide is a pharmacological inhibitor of MLKL with IC50 values of 124 nM in human HT-29, which significantly decreases BV6/DAC-induced cell death in MV4-11 cells. It prevents MLKL-RIP1-RIP3 necrosome complex from interacting with downstream necrosis effectors.
An impurity of Ropinirole. Ropinirole acts as a D2, D3, and D4 dopamine receptor agonist with highest affinity for D2. It is weakly active at the 5-HT2, and α2 receptors and is said to have virtually no affinity for the 5-HT1, GABA, mAChRs, α1, and β-adrenoreceptors.
N-Desmethyl Vandetanib is a metabolite of Vandetanib. Vandetanib is an antitumor drug used for the treatment of medullary thyroid cancer. Vandetanib effects through inhibiting vascular endothelial growth factor receptor-2 (VEGFR), epidermal growth factor receptor (EGFR) and the RET-tyrosine kinase activity.
N-Desmethyl Ulipristal Acetate is a metabolite of Ulipristal. Ulipristal is a selective progesterone receptor modulator (SPRM) used for emergency contraception and uterine fibroid.
N-desmethyl Enzalutamide is a major metabolite of Enzalutamide. Enzalutamide is an androgen-receptor (AR) antagonist (IC50 = 36 nM) in LNCaP cells that inhibits the transcriptional activity of a mutant AR protein. Enzalutamide resists against induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2). N-desmethyl Enzalutamide can be used for the treatment of disorders involving androgen, estrogen and progesterone receptors.
N-Desmethyl Azelastine is the main metabolite of Azelastine. Azelastine is a potent, selective and second-generation histamine antagonist. It inhibits histamine via competing with histamine for the H1 receptor.
A metabolite of Quetiapine. Quetiapine is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.
ND-646 is an orally bioactive inhibitor of acetyl-CoA carboxylase (ACC) that inhibits both ACC1 and ACC2. It prevents ACC subunit dimerization to inhibit fatty acid synthesis in vitro and in vivo.
ND-630, also called as NDI 010976, is a highly selective, reversible inhibitor of acetyl-CoA carboxylase (ACC) and had IC50 values of 2 and 7 nM for ACC1 and 2, respectively, EC50 values in HepG2 serum free and 10% serum of 9 and 66 nM, respectively, and 2-fold C2C12 fatty acid oxidation (FAOxn) stimulation at 200 nM.
N-Cyano-N'-methyl-ethanimidamide has exhibited significant inhibitory activity against the dipeptidyl peptidase IV (DPP-4), which represents a pharmacological target for mitigating type 2 diabetes. In addition to this, the product has demonstrated antiviral potential against a diverse range of viral strains, among which the human immunodeficiency virus (HIV) is notable. The product's diverse clinical applications thus mandate in-depth investigation and analysis.
NCT-503 is a non-competitive phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50= 2.5 µM), reducing the production of glucose-derived serine in cells and suppressing the growth of PHGDH-dependent cancer cells in culture and in orthotopic xenograft tumors.
N-Cocoyl-L-Glutamic Acid is a chemical compound derived from coconut oil. It has surfactant properties, making it useful in the manufacturing of personal care products such as shampoos and cleansing bars.
NCGC00244536 is a potent KDM4A inhibitor (IC50 = 10 nM) that inhibits the in vivo growth of tumors derived from PC3 cells and ex vivo human PCa explants.
N-Benzoyl-5'-O-(4,4'-dimethoxytrityl)-2'-O-methyladenosine-3'-(2-cyanoethyl-N,N-diisopropyl)phosphoramidite (CAS# 110782-31-5) is a nucleotide used in the synthesis of native-like crosslinked duplex RNA.
N-Benzoyl-5'-O-(4,4-Dimethoxytrityl)-2'-O-[(tert-butyl)dimethylsilyl]adenosine-3'-(2-cyanoethyl-N,N-diisopropyl)phosphoramidite is a classic protected 2-OTBDMS phosphoramidite used to incorporate nucleoside A into the synthesis of oligonucleotides.
Navitoclax is an orally active, synthetic small molecule and an antagonist of a subset of the B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity.
