化合物GNE617 T4335

Product Introduction
Bioactivity


英文名: GNE-617

描述: GNE-617 是一种新型的、特异性的Nampt 抑制剂，在A549细胞中IC50为18.9nM。

细胞实验: GNE-617 is dissolved in DMSO and stored, and then diluted with appropriate media before use.Cells are grown in RPMI-1640 medium supplemented with 10% FBS and 2 mM glutamine and passaged not more than 20 times after thawing. To determine the IC50 values and nicotinic acid rescue status, cells are treated with nine point dose titrations of GNE-617 with or without 10 μM nicotinic acid. At 96 hours post-drug addition, the GNE-617-treated cells are evaluated using CyQUANT Direct Cell Proliferation Assay followed by CellTiter-Glo Luminescent Cell Viability Assay quantified with a Wallac EnVision 2104 Multilabel Reader. IC50 values are calculated using XLfit 5.1. To examine the protein level, cells are lysed in ice-cold radioimmunoprecipitation assay buffer, run on SDS-PAGE (4%-12% Bis-Tris), and evaluated by Western blotting using antibodies directed against NAPRT1 and β-actin

激酶实验: For RNA interference (RNAi), A549 cells are plated at 1,500 cells per well in 96-well plates, allowed to adhere for 24 hours, and transfected with 25 nM siRNA oligonucleotide using Dharmafect 4. Transfected cells are treated with the indicated concentrations of GNE-617 (0.1, 1 , 10 , 100 , and 1000 nM) for 72 hours and viability is evaluated with CellTiter-Glo. Lysates for detection of NAPRT1 protein are collected 72 hours after transfection of 1 million A549 cells in 10 cm dishes. For NAPRT1 re-expression, RERF-LC-MS cells are transfected with pCMV6-AC.NAPRT1 and empty vector pCMV6-AC using Amaxa Nucleofector technology and selected with Geneticin

动物实验: Male na?ve Sprague Dawley rats are administered once daily via oral gavage with GNE-617( 30?mg/kg), formulated as a solution in the vehicle of 60% polyethylene glycol (PEG 400)/10% ethanol/30% 5% dextrose in water (D5W) .

体外活性: 在A549细胞中，GNE-617抑制NAMPT（IC50=18.9 nM）。

体内活性: In rats, GNE-617 hydrochloride (administered QD) and GNE-875 (administered BID) are associated with more severe retinal toxicity at similar exposures and dosing duration compared with GMX-1778 (administered BID). The mouse efficacy studies using GNE-617, GNE-618, and GMX-1778 are designed to assess efficacy and opportunistically used to assess retinal toxicity in mice. NAMPTi retinal toxicity is observed with GNE-617 and GMX-1778; nevertheless, the different study durations between GNE-617 and GMX-1778 do not allow for direct comparison of retinal toxicity.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 25 mg/mL (58.49 mM)


关键字: Pre-B cell colony enhancing factor | Inhibitor | GNE 617 | GNE-617 | PBEF | Visfatin | Nicotinamide phosphoribosyl transferase | inhibit | NAMPT

相关产品: NAMPT degrader-3 | Nampt activator-1 | STF-118804 | SBI-797812 | CHS-828 | LB-60-OF61 | OT-82 | Nampt activator-2 | Teglarinad chloride | GNE-618

相关库: Glycometabolism Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Fluorochemical Library | Inhibitor Library | Anti-Cancer Active Compound Library | Metabolism Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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