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134865-74-0

中文名稱 4-P-PDOT
英文名稱 4-P-PDOT
CAS 134865-74-0
分子式 C19H21NO
分子量 279.38
MOL 文件 134865-74-0.mol
更新日期 2024/06/25 17:16:00
134865-74-0 結(jié)構(gòu)式 134865-74-0 結(jié)構(gòu)式

基本信息

中文別名
N-(4-苯基-1,2,3,4-四氫-2-萘基)丙酰胺
英文別名
AH-024
4-P-PDOT
4-PHENYL-2-PROPIONAMIDOTETRALIN
N-(4-phenyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide
N-(4-Phenyl-1,2,3,4-tetrahydronaphthalen-2-yl)propionamide
Propanamide, N-(1,2,3,4-tetrahydro-4-phenyl-2-naphthalenyl)-
4-P-PDOT
4PPDOT
4P-PDOT
AH-024
4-PHENYL-2- PROPIONAMIDOTETRALIN.

物理化學(xué)性質(zhì)

熔點(diǎn)166 °C
沸點(diǎn)480.1±45.0 °C(Predicted)
密度1.11±0.1 g/cm3(Predicted)
儲(chǔ)存條件Store at RT
溶解度Soluble in DMSO > 10 mM
酸度系數(shù)(pKa)15.87±0.40(Predicted)
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302
RTECS號(hào)TX1498350
海關(guān)編碼2924.29.7790

常見問(wèn)題列表

生物活性
4-P-PDOT 是一種有效的,選擇性的和親和性的褪黑激素受體 (MT2) 拮抗劑。4-P-PDOT 對(duì) MT2 的選擇性是 MT1 的 300 倍以上。4-P-PDOT 可顯著抵消褪黑激素介導(dǎo)的抗氧化作用 (GSH/GSSG比,ERK 磷酸化,Nrf2 核易位,Nrf2 DNA 結(jié)合活性)。
靶點(diǎn)

MT2 receptor

體外研究

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.
體內(nèi)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.
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