PS10|cas:1564265-82-2|西域试剂

PS10,99.01%

产品编号：Bellancom-121744| CAS NO：1564265-82-2| 分子式：C₁₄H₁₃NO₆S| 分子量：323.32

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货号	价格	库存与货期
Bellancom-121744	￥1000.00	杭州北京（现货）
Bellancom-121744	￥1800.00	杭州北京（现货）
Bellancom-121744	￥6700.00	杭州北京（现货）
Bellancom-121744	￥11000.00	杭州北京（现货）

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PS10

产品介绍

PS10 是一种新型，有效且具有 ATP 竞争性的广谱 PDK 抑制剂，可抑制所有 PDK 同工型，对 PDK2，PDK4，PDK1 和 PDK3 的 IC₅₀ 分别为 0.8 μM，0.76 μM，2.1 μM 和 21.3 μM。 PS10 对 PDK2 (K_d= 239 nM) 的亲和力高于对 Hsp90 (K_d= 47 μM)。 PS10 改善葡萄糖耐量，刺激饮食引起的肥胖症中的心肌碳水化合物氧化。 PS10 具有研究糖尿病性心肌病的潜力。

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 (K_d= 239 nM) than for Hsp90 (K_d= 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

体外研究

PS10 shows a higher affinity of PS10 for PDK2 (K_d= 239 nM) than for Hsp90 (K_d= 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

PS10 (Intraperitoneal injection; 70 mg/kg; single dose) treatment lead to 11- and 23-fold higher PDC activity in heart and liver, respectively. Meanwhile, there results in a 1.4-fold enhancement of PDC activity in kidneys 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 shows similar glucose tolerance response to glucose challenge restores PDC activity in the DIO mouse hearts.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (193.31 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0929 mL	15.4646 mL	30.9291 mL
5 mM	0.6186 mL	3.0929 mL	6.1858 mL
10 mM	0.3093 mL	1.5465 mL	3.0929 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 6.25 mg/mL (19.33 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (19.33 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 6.25 mg/mL (19.33 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (19.33 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明