4-Thio-UTP是UTP的类似物，也是强效P2Y2和P2Y4受体激动剂，对hP2Y2和hP2Y4 的EC50分别为35nM和350nM。
Sample solution is provided at 25 µL, 10mM.
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4-Thio-UTP is a UTP analog and potent P2Y2 and P2Y4 agonist with EC50 values of 35 and 350nM for hP2Y2 and hP2Y4, respectively[1]. P2Y2 and P2Y4 are G-protein-coupled purinergic receptors activated extracellularly by UTP that mobilize intracellular Ca²⁺ and thereby regulate epithelial ion/water transport, immune cell recruitment and vascular tone[2]. 4-Thio-UTP is widely used to investigate purinergic signaling in inflammation, epithelial ion transport, neurotransmission, and immune regulation[3]. 4-Thio-UTP is also used in cross-linking experiments and for labeling transcription complexes to explore the behavior of RNA polymerase during transcription elongation and termination[4].
In vitro, 4-Thio-UTP (0.1-300μM; 20min) evoked a concentration-dependent accumulation of [³H]inositol polyphosphates in cultured rat aortic smooth muscle cells[5].
In vivo, 4-Thio-UTP (100μM; 15min; basolateral perfusion) stimulated chloride secretion in wild-type mouse jejunum and the response was attenuated in both P2Y4-and P2Y2-deficient mice[6]. 4-Thio-UTP (0.44mg/kg; i.v.; 30min before LAD ligation) reduced myocardial infarct size and improved left-ventricular fractional shortening in wild-type mice but lost protection in P2Y2⁻/⁻mice[7].
References:
[1] Jacobson KA, Costanzi S, Ivanov AA, et al. Structure activity and molecular modeling analyses of ribose- and base-modified uridine 5'-triphosphate analogues at the human P2Y2 and P2Y4 receptors. Biochem Pharmacol. 2006;71(4):540-549.
[2] Hede SE, Amstrup J, Klaerke DA, Novak I. P2Y2 and P2Y4 receptors regulate pancreatic Ca(2+)-activated K+ channels differently. Pflugers Arch. 2005;450(6):429-436.
[3] Lazarowski ER, Boucher RC. UTP as an extracellular signaling molecule. News Physiol Sci. 2001;16:1-5.
[4] Bartholomew B, Dahmus ME, Meares CF. RNA contacts subunits IIo and IIc in HeLa RNA polymerase II transcription complexes. J Biol Chem. 1986;261(30):14226-14231.
[5] Kumari R, Goh G, Ng LL, Boarder MR. ATP and UTP responses of cultured rat aortic smooth muscle cells revisited: dominance of P2Y2 receptors. Br J Pharmacol. 2003;140(7):1169-1176.
[6] Ghanem E, Robaye B, Leal T, et al. The role of epithelial P2Y2 and P2Y4 receptors in the regulation of intestinal chloride secretion. Br J Pharmacol. 2005;146(3):364-369.
[7] Cohen R, Shainberg A, Hochhauser E, et al. UTP reduces infarct size and improves mice heart function after myocardial infarct via P2Y2 receptor. Biochem Pharmacol. 2011;82(9):1126-1133.
4-Thio-UTP是UTP的类似物，也是强效P2Y2和P2Y4受体激动剂，对hP2Y2和hP2Y4 的EC50分别为35nM和350nM[1]。P2Y2与P2Y4是经UTP激活的G蛋白偶联嘌呤能受体，可动员细胞内Ca²⁺，进而调节上皮离子/水的转运、免疫细胞募集及血管张力[2]。4-Thio-UTP被广泛用于研究炎症、上皮离子转运、神经传递和免疫调节中的嘌呤能信号[3]。4-Thio-UTP也用于交联实验和标记转录复合体，以探索RNA聚合酶在转录延伸与终止过程中的行为[4]。
体外研究表明，4-Thio-UTP（0.1-300μM；20min）可在培养的大鼠主动脉平滑肌细胞中浓度依赖性地诱导[³H]肌醇多磷酸积聚[5]。
体内实验中，4-Thio-UTP（100μM；15min；基底侧灌流）可刺激野生型小鼠空肠的氯离子分泌，且在P2Y4或P2Y2缺失小鼠中该反应减弱[6]。4-Thio-UTP（0.44mg/kg；结扎前30min静脉注射）可缩小心肌梗死面积并改善野生型小鼠左室短轴缩短率，而在P2Y2⁻/⁻小鼠中失去保护作用[7]。
| Cell experiment [1]: | |
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Cell lines |
rat aortic smooth muscle cells |
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Preparation Method |
Rat aortic VSMCs from both spontaneously hypertensive (SHR) and normotensive (WKY) animals were prepared according to protocol. For the total [3H]-inositol (poly)phosphate measurements, cells were culturedto 80% confluence in 24-well multi-well plates. The medium was then replaced with 500μl of serumfree M199 medium supplemented with 50IU/ml penicillin, 50μg/ml streptomycin, 2mM L-glutamine and1μCi/ml(0.037MBq/ml) D-myo-[2-3H]inositol. After 24h, cells were incubated with 10mM LiCl for 10min – where appropriate suramin was included with the lithium. After 20min stimulation with 4-Thio-UTP (0.1-300μM) in the continuing presence of lithium, the reaction was stoppedwith trichloroacetic acid, the solution was neutralised with freon : octylamine extraction, and addition of NaHCO3 and[3H]inositol phosphates separatedon small Dowex-1 columns. |
|
Reaction Conditions |
0.1-300μM; 20min |
|
Applications |
4-Thio-UTP evoked a concentration-dependent accumulation of [³H]inositol polyphosphates in cultured rat aortic smooth muscle cells. |
| Animal experiment [2]: | |
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Animal models |
P2Y2⁻/⁻ and P2Y4⁻/⁻ mice; DF508 mice |
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Preparation Method |
P2Y2⁻/⁻ and P2Y4⁻/⁻ mice and their littermates were maintained on a standard diet in conventional facilities. DF508 mice and their littermates were weaned to a liquid diet and the colony was maintained in a pathogen-free status. Mice were kept in a 12-h light–dark cycle. chloride secretion was assessed as the Isc following addition of phloridzin or amiloride to the apical side as well as of indomethacin (100μM) to both bathing media. 4-Thio-UTP was added, at 100μM, to the apical or basolateral solution, unless otherwise stated. Forskolin was always added to the basolateral solution at the concentration of 10μM in ethanol 0.1%; this concentration of ethanol does not affect Isc. The increase in Isc was calculated as the difference between the basal current and the peak current obtained within 15min of addition of 4-Thio-UTP or forskolin. Statistical analysis was performed using the unpaired t-test and a P-value |
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Dosage form |
100μM; 15min; basolateral perfusion |
|
Applications |
4-Thio-UTP stimulated chloride secretion in wild-type mouse jejunum and the response was attenuated in both P2Y4- and P2Y2-deficient mice. |
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References: |
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| Cas No. | SDF | Download SDF | |
| 分子式 | C9H15N2O14P3S (free acid) | 分子量 | 500.2 (free acid) |
| 溶解度 | 储存条件 | Store at -20°C or below | |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9992 mL | 9.996 mL | 19.992 mL |
| 5 mM | 399.8 μL | 1.9992 mL | 3.9984 mL |
| 10 mM | 199.9 μL | 999.6 μL | 1.9992 mL |
Quality Control & SDS
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- Purity: >96.00% Appearance: A soluble in water
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