Ertiprotafib PTP 112|cas:251303-04-5|西域试剂

Ertiprotafib PTP 112,98.86%

产品编号：Bellancom-19383| CAS NO：251303-04-5| 分子式：C₃₁H₂₇BrO₃S| 分子量：559.51

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货号	价格	库存与货期
Bellancom-19383	￥3500.00	杭州北京（现货）
Bellancom-19383	￥6000.00	杭州北京（现货）
Bellancom-19383	￥12500.00	杭州北京（现货）

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Ertiprotafib PTP 112

产品介绍

Ertiprotafib 是 PTP1B， IKK-β 的抑制剂，其 IC₅₀ 值分别是 1.6 μM，400 nM，同时也是PPARα/PPARβ 的激动剂，其 EC₅₀ 值为 ~1 μM。

生物活性

Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC₅₀ of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC₅₀ of ~1 μM for PPARα/PPARβ.

体外研究

Ertiprotafib is a potent inhibitor of IKK-β, with an IC₅₀ value of 400±40 nM, which is much lower than that required for the half-maximal inhibition of the p-nitrophenyl phosphatase activity of PTP1B. The reported IC₅₀ value of Ertiprotafib against PTP1B ranges from 1.6 to 29 μM depending on the assay conditions. Ertiprotafib is at least a dual PPARα and PPARβ agonist with EC₅₀ values for transactivation of 1 μM. Such activities readily explain the observations with suprapharmacologic doses of these.

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

体内研究

As seen with treatment of ob/ob mice, both Ertiprotafib and compound 3 seem to significantly improve glucose metabolism in rats. At 25 mg/kg/day, these compounds decrease both fasting blood glucose and insulin levels compared with vehicle treated rats. Furthermore, both Ertiprotafib and compound 3 increase glucose disposal after an oral challenge. It is noteworthy that lipid levels are also reduced in treated animals. Both triglyceride and free fatty acid levels are substantially reduced in rats treated with 25 mg/kg/day of either compound. To summarize, both Ertiprotafib and compound 3 seem to be robust agents in improving glucose utilization in fa/fa rats while also decreasing lipid levels in these animals. Decreased lipid levels may be unexpected for a pure PTP1b inhibitor. It is more telling, as mentioned above, that rats treated with suprapharmacologic doses of Ertiprotafib show signs of PPAR family activation.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (178.73 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7873 mL	8.9364 mL	17.8728 mL
5 mM	0.3575 mL	1.7873 mL	3.5746 mL
10 mM	0.1787 mL	0.8936 mL	1.7873 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 (sealed storage, away from moisture and light)。-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: 2.5 mg/mL (4.47 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.47 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 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% corn oil
Solubility: ≥ 2.5 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.47 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。