- AR-C155858
| UK-5099MCTs and MPC inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 99.41%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
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| Cas No. | 56396-35-1 | SDF | Download SDF |
| Synonyms | PF-1005023;UK5099;UK 5099;PF1005023;PF 1005023 | ||
| Chemical Name | (E)-2-cyano-3-(1-phenylindol-3-yl)prop-2-enoic acid | ||
| Canonical SMILES | C1=CC=C(C=C1)N2C=C(C3=CC=CC=C32)C=C(C#N)C(=O)O | ||
| Formula | C18H12N2O2 | M.Wt | 288.3 |
| Solubility | ≥28.8 mg/mL in DMSO, <2.38 mg/ml="" in="" etoh,=""><2.44 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier [1]. The mitochondrial pyruvate carrier (MPC) facilitates pyruvate transport across the mitochondrial inner membrane and plays a critical role in carbohydrate, lipid and amino acid metabolism.UK-5099 (1 mM) completely blocked pyruvate uptake with Ki value of 49 μM. Also, UK-5099 decreased the overall efflux rate in a concentration-dependant way [1]. In mitochondria isolated from S. Guttatum, UK-5099 (20 μM) inhibited pyruvate-dependent 02 consumption [2]. In rat heart mitochondria, UK-5099 inhibited pyruvate oxidation with a non-linear inhibition kinetics [2]. In glucagon-treated rats, UK-5099 inhibited pyruvate carboxylation and total pyruvate metabolism with a linear relationship [3]. In rat liver and heart mitochondria, UK-5099 inhibited pyruvate-dependent 02 consumption with IC50 value of 50 nM [4].References:[1]. Wiemer EA, Michels PA, Opperdoes FR. The inhibition of pyruvate transport across the plasma membrane of the bloodstream form of Trypanosoma brucei and its metabolic implications. Biochem J, 1995, 312 ( Pt 2): 479-484.[2]. Halestrap AP. The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors. Biochem J, 1975, 148(1): 85-96.[3]. Halestrap AP, Armston AE. A re-evaluation of the role of mitochondrial pyruvate transport in the hormonal control of rat liver mitochondrial pyruvate metabolism. Biochem J, 1984, 223(3): 677-685.[4]. Proudlove MO, Beechey RB, Moore AL. Pyruvate transport by thermogenic-tissue mitochondria. Biochem J, 1987, 247(2): 441-447.
