4-P-PDOT

4-P-PDOT

中文名称4-P-PDOT
中文同义词N-(4-苯基-1,2,3,4-四氢-2-萘基)丙酰胺;4-P-PDOT,MT 2褪黑激素受体拮抗剂
英文名称4-P-PDOT
英文同义词4-PHENYL-2-PROPIONAMIDOTETRALIN;4-P-PDOT;N-(4-phenyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide;4-P-PDOT; 4PPDOT; 4P-PDOT; AH-024; 4-PHENYL-2- PROPIONAMIDOTETRALIN.;AH-024;Propanamide, N-(1,2,3,4-tetrahydro-4-phenyl-2-naphthalenyl)-;N-(4-Phenyl-1,2,3,4-tetrahydronaphthalen-2-yl)propionamide;Melatonin,Melatonin Receptor,GSSG,Nrf2,GSH,4PPDOT,ERK,memory,damage,Inhibitor,oxidative,4 P PDOT,MT2,inhibit
CAS号134865-74-0
分子式C19H21NO
分子量279.38
EINECS号
相关类别Melatonin receptor
Mol文件134865-74-0.mol
结构式4-P-PDOT 结构式

4-P-PDOT 性质

熔点166 °C
沸点480.1±45.0 °C(Predicted)
密度1.11±0.1 g/cm3(Predicted)
储存条件room temp
溶解度溶于 DMSO > 10 mM
酸度系数(pKa)15.87±0.40(Predicted)
形态粉末
颜色白色至米色

4-P-PDOT 用途与合成方法

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)。

MT2 receptor

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 pEC 50 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.

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.

安全信息

RTECS号TX1498350
海关编码2924.29.7790

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30P25874-P-PDOT
4-P-PDOT
134865-74-05mg290元
2024/04/30P25874-P-PDOT
4-P-PDOT
134865-74-025mg735元

4-P-PDOT 上下游产品信息

"4-P-PDOT"相关产品信息
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