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UK-5099
🥰Excellent
Catalog No. T4441Cas No. 56396-35-1
Alias UK5099, UK 5099, PF-1005023
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].
UK-5099
🥰Excellent
Purity: 100%
Catalog No. T4441Alias UK5099, UK 5099, PF-1005023Cas No. 56396-35-1
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].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $30 | In Stock | |
| 5 mg | $62 | In Stock | |
| 10 mg | $89 | In Stock | |
| 25 mg | $177 | In Stock | |
| 50 mg | $296 | In Stock | |
| 100 mg | $449 | In Stock | |
| 500 mg | $987 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $71 | In Stock |
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Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | 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]. |
| Targets&IC50 | MPC:50 nM |
| In vitro | 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]. |
| In vivo | UK5099 increases the glucose excursion seen during an intraperitoneal glucose tolerance test in C57BLK mice[4]. |
| Cell Research | 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]. |
| Animal Research | 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]. |
| Alias | UK5099, UK 5099, PF-1005023 |
| Molecular Weight | 288.3 |
| Formula | C18H12N2O2 |
| Cas No. | 56396-35-1 |
| Smiles | OC(=O)C(=Cc1cn(-c2ccccc2)c2ccccc12)C#N |
| Relative Density. | 1.20 g/cm3 |
Storage & Solubility Information
| Storage | 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. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 16.67 mg/mL (57.81 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1.67 mg/mL (5.79 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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