DPM-1001 trihydrochloride|西域试剂

DPM-1001 trihydrochloride,98.0%

产品编号：Bellancom-121515A| 分子式：C₃₅H₆₀Cl₃N₃O₃| 分子量：677.23

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-121515A		￥9500.00	杭州北京（现货）
Bellancom-121515A		￥16000.00	杭州北京（现货）

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DPM-1001 trihydrochloride

产品介绍

DPM-1001 trihydrochloride 是一种有效的，特异性的，具有口服活性的，且非竞争性的蛋白酪氨酸磷酸酶 (PTP1B) 抑制剂，其 IC₅₀ 为 100 nM。DPM-1001 trihydrochloride 是特异性 PTP1B 抑制剂 MSI-1436 (IC₅₀=600 nM) 的类似物。DPM-1001 trihydrochloride 具有抗糖尿病特性。

生物活性

DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC₅₀ of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property.

体外研究

DPM-1001 trihydrochloride inhibits the short form of PTP1B reversibly, whereas PTP1B(1–405) remained inactive over an extended period of time. DPM-1001 is against PTP1B(1–405) with no pre-incubation, the IC₅₀ value for PTP1B(1–405) is 600 nM. However, after a 30-min pre-incubation, the potency is improved to 100 nM. In contrast, there is no obvious time-dependent change in the IC₅₀ value for PTP1B(1–321).

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

体内研究

DPM-1001 trihydrochloride (oral or intraperitoneal administration; 5 mg/kg; once daily; 50 days) inhibits diet-induced obesity in mice by improving insulin and leptin signaling. DPM-1001 trihydrochloride-treated, high-fat diet-fed mice starts losing weight within 5 days of treatment. The weight loss continues for approximately 3 weeks, after which no further decrease in body weight is observed.

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

Animal Model:	18 weeks of age, high-fat diet (HFD)-fed obese male mice (C57bl6/J)
Dosage:	5 mg/kg
Administration:	Oral or intraperitoneal administration; 5 mg/kg; once daily; 50 day
Result:	Led to an 5% decrease in body weight. Improved glucose tolerance and insulin sensitivity in glucose tolerance and insulin tolerance in vivo.

体内研究

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

Animal Model:	18 weeks of age, high-fat diet (HFD)-fed obese male mice (C57bl6/J)
Dosage:	5 mg/kg
Administration:	Oral or intraperitoneal administration; 5 mg/kg; once daily; 50 day
Result:	Led to an 5% decrease in body weight. Improved glucose tolerance and insulin sensitivity in glucose tolerance and insulin tolerance in vivo.

性状

Solid

溶解性数据

In Vitro:

DMSO : 80 mg/mL (118.13 mM; Need ultrasonic)

H₂O : 33.33 mg/mL (49.22 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4766 mL	7.3830 mL	14.7660 mL
5 mM	0.2953 mL	1.4766 mL	2.9532 mL
10 mM	0.1477 mL	0.7383 mL	1.4766 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 (stored under nitrogen)。-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: ≥ 5 mg/mL (7.38 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (7.38 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (7.38 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (7.38 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (7.38 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (7.38 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。