产品
编 号：F622734
分子式：C14H13NO6S
分子量：323.32
分子式：C14H13NO6S
分子量：323.32
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1564265-82-2
产品详情
生物活性：
PS10 is a novel, potent and ATP-competitive pan-PDK?inhibitor, inhibits all PDK isoforms with?IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
体内研究：
PS10 (Intraperitoneal injection; 70 mg/kg; single dose) treatmentlead to11- and 23-fold higher PDC activity in heart and liver, respectively. Meanwhile, there results in a 1.4-fold enhancement of PDC activity inkidneys compared with vehicle-group.PS10 (Intraperitoneal injection; 70 mg/kg; 3 days) treatment results that thePDC activity profiles and the phospho-E1α subunit level is similar to the single-dose. Notably, the three-day treatment attenuates the enhancement of PDK activity in heart.PS10 (intraperitoneal injection; 70 mg/kg; 4 weeks) is treated in mice and subjected to a glucose tolerance test. when challenged with 1.5 g/kg glucose, the plasma glucose level in the vehicle-treated control is at 200 mg/dl at 0 min, peaks at 482 mg/dl at 30 min, and reduces to 210 mg/dl at 120 min. In PS10-treated DIO mice, the glucose level at 168 mg/dl at 0 min is lower than that in vehicle-treated animals, reachs 312 mg/dl at 30 min, and returns to 163 mg/dl at 120 min.PS10 (intraperitoneal injection; 70 mg/kg) and DCA both stimulates flux through PDC as measured by the appearance of hyperpolarized [13C]bicarbonate. It showssimilar glucose tolerance response to glucose challenge restores PDC activity in the DIO mouse hearts.Animal Model:C57BL/6J male mice at 6 to 8 weeks old
Dosage:70 mg/kg/day
Administration:Intraperitoneal injection
Result:Improved glucose tolerance in the intact animal.
体外研究：
PS10 shows a higher affinity of PS10 for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47,000 nM).PS10 is less potent than cycloheximide in HeLa cells, it shows an IC50 value of 284 μM?for the growth inhibition and PS10 has low toxicity in cells.
PS10 is a novel, potent and ATP-competitive pan-PDK?inhibitor, inhibits all PDK isoforms with?IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
体内研究：
PS10 (Intraperitoneal injection; 70 mg/kg; single dose) treatmentlead to11- and 23-fold higher PDC activity in heart and liver, respectively. Meanwhile, there results in a 1.4-fold enhancement of PDC activity inkidneys compared with vehicle-group.PS10 (Intraperitoneal injection; 70 mg/kg; 3 days) treatment results that thePDC activity profiles and the phospho-E1α subunit level is similar to the single-dose. Notably, the three-day treatment attenuates the enhancement of PDK activity in heart.PS10 (intraperitoneal injection; 70 mg/kg; 4 weeks) is treated in mice and subjected to a glucose tolerance test. when challenged with 1.5 g/kg glucose, the plasma glucose level in the vehicle-treated control is at 200 mg/dl at 0 min, peaks at 482 mg/dl at 30 min, and reduces to 210 mg/dl at 120 min. In PS10-treated DIO mice, the glucose level at 168 mg/dl at 0 min is lower than that in vehicle-treated animals, reachs 312 mg/dl at 30 min, and returns to 163 mg/dl at 120 min.PS10 (intraperitoneal injection; 70 mg/kg) and DCA both stimulates flux through PDC as measured by the appearance of hyperpolarized [13C]bicarbonate. It showssimilar glucose tolerance response to glucose challenge restores PDC activity in the DIO mouse hearts.Animal Model:C57BL/6J male mice at 6 to 8 weeks old
Dosage:70 mg/kg/day
Administration:Intraperitoneal injection
Result:Improved glucose tolerance in the intact animal.
体外研究：
PS10 shows a higher affinity of PS10 for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47,000 nM).PS10 is less potent than cycloheximide in HeLa cells, it shows an IC50 value of 284 μM?for the growth inhibition and PS10 has low toxicity in cells.
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