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
- 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
- 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)。
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靶点
MT2 receptor
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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.
- 更新日期：2024/11/08
- 产品编号：HY-100609
- 产品名称：4-P-PDOT 4-P-PDOT
- CAS编号：134865-74-0
- 包装：5mg
- 价格：900元
- 更新日期：2024/11/08
- 产品编号：HY-100609
- 产品名称：4-P-PDOT 4-P-PDOT
- CAS编号：134865-74-0
- 包装：10mM * 1mLin DMSO
- 价格：990元
- 公司名称：BIOTREND GmbH
- 联系电话：--
- 电子邮件：jaeger@biotrend.com
- 国家：德国
- 产品数：249
- 优势度：65
- 公司名称：BIOTREND Chemicals AG
- 联系电话：--
- 电子邮件：info@biotrend.ch
- 国家：德国
- 产品数：1250
- 优势度：62
- 公司名称：Service Chemical Inc.
- 联系电话：--
- 电子邮件：sales@chemos-group.com
- 国家：德国
- 产品数：6350
- 优势度：71
