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Postion:Product Catalog >UK-5099
UK-5099
  • UK-5099

UK-5099 NEW

Price $30 $62 $89
Package 1mg 5mg 10mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-15

Product Details

Product Name: UK-5099 CAS No.: 56396-35-1
Purity: 97.39% Supply Ability: 10g
Release date: 2024/11/15

Product Introduction

Bioactivity

名稱UK-5099
描述UK-5099 (PF-1005023) is a specific and potent inhibitor of MPC carrier activity, effectively inhibiting pyruvate-dependent oxygen consumption in rat heart mitochondria with an IC50 of 50 nM [1].
細(xì)胞實(shí)驗(yàn)The 832/13 cell line derived from INS-1 rat insulinoma cells is used for experiments. Cell viability is measured using CellTiter Blue. The assay is based on the cellular reduction of resazurin to resorufin. The appearance of resorufin is monitored by fluorescence emission at 585 nm using a Spectramax M5 microplate reader with excitation at 555 nm. For UK5099-treated cells, cells are allowed to recover for 1 h before measuring cell viability. Data are expressed as -fold relative to no treatment or siCtrl[4].
動物實(shí)驗(yàn)C57BLK mice are fasted for 16 h prior to glucose challenge. UK5099 (32 μmol/kg of body weight) or DMSO in PBS is injected into the intraperitoneal cavity 30 min before injecting glucose (1.5 mg of glucose/g of body weight). Blood glucose levels are measured at 0, 10, 20, 30, 60, and 120 min after glucose injection[4].
體外活性The trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (Ki: 17 mM) but can be completely blocked by UK-5099 (Ki: 49 μM)[2]. UK-5099 also inhibits the monocarboxylate transporter (MCT) [3]. UK5099 dose-dependently significantly inhibits the glucose-stimulated rise in oxygen consumption and at 150 μM reduced oxygen consumption below basal levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells[4]. The UK5099 treated cells show a significantly higher proportion of side population fraction and express higher levels of stemness markers Oct3/4 and Nanog. The UK5099 application may be an ideal model for Warburg effect studies[5].
體內(nèi)活性UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice[4].
存儲條件store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 16.67 mg/mL (57.81 mM), Sonication is recommended.
關(guān)鍵字UK-5099 | PF1005023 | PF 1005023 | Mitochondrial Metabolism | Inhibitor | inhibit
相關(guān)產(chǎn)品Imeglimin hydrochloride | Rotenone | Glibenclamide | α-Lipoic Acid | Tricarballylic acid | Boscalid | α-Lipoic Acid | (-)-Epigallocatechin Gallate | Lipoic acid | CCCP | D-Histidine | Nerol
相關(guān)庫銅死亡化合物庫 | 細(xì)胞重編程化合物庫 | 糖代謝化合物庫 | 經(jīng)典已知活性庫 | 抑制劑庫 | 線粒體靶向庫 | NO PAINS 化合物庫 | 代謝化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 共價(jià)抑制劑庫

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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