4-P-PDOT
目录号 : KM4352 CAS No. : 134865-74-0 纯度 : 98%

4-P-PDOT 是一种有效的,选择性的和亲和性的褪黑激素受体 (MT2) 拮抗剂。4-P-PDOT 对 MT2 的选择性是 MT1 的 300 倍以上。4-P-PDOT 可显着抵消褪黑激素介导的抗氧化作用 (GSH/GSSG比,ERK 磷酸化,Nrf2 核易位,Nrf2 DNA 结合活性)。

规格 价格 是否有货 数量
1mg
In-stock
5mg
In-stock
10mg 询价 In-stock
50mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity).

体外研究

In CHO-mt1 cells the amidotetraline 4-P-PDOT (10 mM) has no effect on forskolin-stimulated cyclic AMP levels, either alone, or in the presence of Melatonin. In contrast, in CHO-MT2 cells, 4-P-PDOT is an agonist, producing a concentration-dependent inhibition of forskolin stimulated cyclic AMP, with a pEC50 value of 8.72 and intrinsic activity of 0.86.

Cell Viability Assay

Cell Line: HT-29 and HeLa cells.
Concentration: 30 min.
Incubation Time: 50 µM.
Result: Produced a negligible effect on cell viability induced by melatonin.
体内研究

4-P-PDOT (0.5-1.0 mg/kg; intravenous injection; klotho mutant mice) treatment significantly reverses antioxidant effects mediated by Melatonin. And significantly reverses the changes in the levels of these GSH-related parameters. 4-P-PDOT treatment significantly reverses the memory function of Melatonin-treated klotho mutant mice. 4-P-PDOT also counteracts Melatonin-mediated attenuation in response to the decreases in phospho-ERK expression, Nrf2 nuclear translocation, Nrf2 DNA-binding activity, and GCL mRNA expression in the hippocampi of klotho mutant mice.

Animal Model: Klotho mutant mice treatment with Melatonin
Dosage: 0.5 mg/kg or 1.0 mg/kg
Administration: Intravenous injection
Result: Significantly reversed antioxidant effects mediated by Melatonin. Significantly reversed the changes in the levels of these GSH-related parameters. Significantly reversed the memory function of Melatonin-treated klotho mutant mice.
分子式
C19H21NO
分子量
279.38
CAS号
134865-74-0
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 41.67 mg/mL (149.15 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5794 mL 17.8968 mL 35.7935 mL
5 mM 0.7159 mL 3.5794 mL 7.1587 mL
10 mM 0.3579 mL 1.7897 mL 3.5794 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 4.17 mg/mL (14.93 mM); Clear solution

    此方案可获得 ≥ 4.17 mg/mL (14.93 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 41.7 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 4.17 mg/mL (14.93 mM); Clear solution

    此方案可获得 ≥ 4.17 mg/mL (14.93 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 41.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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