4-P-PDOT

生物活性靶点体外研究体内研究 4-P-PDOT 试剂级价格

4-P-PDOT

CAS号:134865-74-0
英文名:4-P-PDOT
中文名:4-P-PDOT
CBNumber:CB7203987
分子式:C19H21NO
分子量:279.38
MOL File:134865-74-0.mol

4-P-PDOT化学性质

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 :Soluble in DMSO > 10 mM
酸度系数(pKa) :15.87±0.40(Predicted)
形态 :powder
颜色 :white to beige

安全信息

RTECS号 :TX1498350
海关编码 :2924.29.7790

4-P-PDOT性质、用途与生产工艺

生物活性 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)。
靶点

MT2 receptor

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 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.

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.