二芳基丙腈（DPN）（Diarylpropionitrile）是一种非甾体雌激素受体β； (ERβ) 选择性配体，EC50 为 0.85 nM。
| Cas No. | 1428-67-7 |
| 别名 | 2,3-双(4-羟苯基)丙腈,diarylpropionitrile |
| 化学名 | (R)-2,3-bis(4-hydroxyphenyl)propanenitrile |
| Canonical SMILES | OC1=CC=C(C=C1)[C@H](C#N)CC(C=C2)=CC=C2O |
| 分子式 | C15H13NO2 |
| 分子量 | 239.27 |
| 溶解度 | DMSO : 100 mg/mL (417.94 mM) |
| 储存条件 | Desiccate at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 文献引用 | |
| 产品描述 | DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β(ER β) selective ligand.IC50 value:Target: ER β ligandin vitro: Pre-treatment with 1-100 nM DPN significantly decreased neuronal cell death by increasing cell viability through a significant attenuation in the reactive oxygen species level, downregulation of pro-apoptotic activated caspase-3 and Bax, and upregulation of anti-apoptotic Bcl-2, thereby mitigating apoptotic morphological alterations. DPN pre-treatment decreased the expression levels of pro-inflammatory cytokines IL-1β and IL-6 through attenuation of Aβ1-42-induced phosphorylation of mitogen-activated protein kinases JNK and p38. In addition, DPN enhanced ERK1/2 and Akt phosphorylation depressed by Aβ1-42 [1]. ERβ was expressed in RAW264.7 cells, and DPN statistically significantly decreased LPS-induced RANTES production in RAW264.7 cells. Small interfering RNA targeting the ERβ gene inhibited the effect of DPN on RANTES production. In addition, DPN inhibited nuclear translocation and phosphorylation of p65 by inhibiting IκB degradation and thus prohibited the activation of nuclear factor κB (NF-κB) [3].in vivo: DPN treatment during EAE did not attenuate demyelination, only partially improved axon conduction, and did not activate the phosphatidylinositol 3-kinase/serine-threonine-specific protein kinase/mammalian target of rapamycin signaling pathway in ERβ CKO mice [2]. References:
[1]. Suwanna N, et al. Neuroprotective effects of diarylpropionitrile against β-amyloid peptide-induced neurotoxicity in rat cultured cortical neurons. Neurosci Lett. 2014 Aug 22;578:44-9.
[2]. Khalaj AJ, et al. Estrogen receptor (ER) β expression in oligodendrocytes is required for attenuation of clinical disease by an ERβ ligand. Proc Natl Acad Sci U S A. 2013 Nov 19;110(47):19125-30.
[3]. Huang SY, et al. Estrogen receptor β agonist diarylpropionitrile inhibits lipopolysaccharide-induced regulated on activation normal T cell expressed and secreted (RANTES) production in macrophages by repressing nuclear factor κB activation. Fertil Steril. 2013 Jul;100(1):234-40. |
