KY-226 是一种有效的,选择性的,口服活性的和变构蛋白酪氨酸磷酸酶 1B (PTP1B) 抑制剂,IC50为 0.25 μM,且不激活 PPARγ 。KY-226 通过增强胰岛素和瘦素信号传导发挥抗糖尿病和抗肥胖作用。KY-226 还可以保护神经元免受脑缺血损伤。
生物活性 | KY-226 is a potent, selective, orally active and allostericprotein tyrosinephosphatase1B (PTP1B)inhibitor with anIC50of 0.25 μM, and withoutPPARγ agonistactivity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancinginsulinandleptinsignaling, respectively. KY-226 also protects neurons from cerebral ischemic injury[1][2]. |
IC50& Target | IC50: 0.25 μM (Protein tyrosine phosphatase 1B (PTP1B))[2] |
体外研究 (In Vitro) | In human hepatoma-derived cells (HepG2), KY-226 (0.3-10 μM) increases the phosphorylated insulin receptor (pIR) produced by insulin[1]. KY-226 (1 μM; 24 hours; bEnd.3 cells) treatment rescues lipopolysaccharide-induced reduction of mRNA and protein levels of ZO-1. KY-226 treatment restores phosphorylation of pAkt (T308) and its downstream target forkhead box protein O1 (FoxO1) (S256) in bEnd.3 cells[2].
Western Blot Analysis[1] Cell Line: | bEnd.3 cells stimulated with LPS | Concentration: | 1 μM | Incubation Time: | 24 hours | Result: | Rescued lipopolysaccharide-induced reduction of mRNA and protein levels of ZO-1. |
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体内研究 (In Vivo) | KY-226 (10-30 mg/kg/day; oral administration; daily; for 4 weeks; maledb/dbmice) treatment significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain[1]. KY-226 attenuates plasma glucose elevations in the oral glucose tolerance test. KY-226 also increases pIR and phosphorylated Akt in the liver and femoral muscle[1].
Animal Model: | Maledb/dbmice (8-11 weeks old)[1] | Dosage: | 10 mg/kg and 30 mg/kg | Administration: | Oral administration; daily; for 4 weeks | Result: | Significantly reduced plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(519.03 mM;Need ultrasonic) 配制储备液 1 mM | 2.0761 mL | 10.3806 mL | 20.7611 mL | 5 mM | 0.4152 mL | 2.0761 mL | 4.1522 mL | 10 mM | 0.2076 mL | 1.0381 mL | 2.0761 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: ≥ 2.08 mg/mL (4.32 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.32 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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