Diarylpropionitrile - CAS 1428-67-7
Catalog number: 1428-67-7
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Estrogen Receptor/ERR
Diarylpropionitrile, also called as DPN, is a selective agonist of estrogen receptor β (ERβ) with a 70-fold higher relative binding affinity for ERβ(18%) versus ER (0.25%). ERβ: EC50 = 0.85 nM; ERα: EC50 = 66 nM
>99 %
White powder
Soluble to 30 mM in 1eq. NaOH, to 100 mM in ethanol, to 100 mM in DMSO, to ~30 mg/ml in DMF, and to 0.5 mg/ml at 25 °C in water
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -37℃ for long term (months to years).
Shelf Life:
2 years
1.256 g/cm3
Canonical SMILES:
1.Estrogen receptor β activation stimulates the development of experimental autoimmune thyroiditis through up-regulation of Th17-type responses.
Qin J;Li L;Jin Q;Guo D;Liu M;Fan C;Li J;Shan Z;Teng W Clin Immunol. 2018 May;190:41-52. doi: 10.1016/j.clim.2018.02.006. Epub 2018 Feb 23.
Estrogens play important roles in autoimmune thyroiditis, but it remains unknown which estrogen receptor (ER) subtype mediates the stimulatory effects. Herein we treated ovariectomized mice with ERα or ERβ selective agonist followed by thyroglobulin-immunization to induce experimental autoimmune thyroiditis (EAT), and observed the aggravation of EAT after diarylpropionitrile (DPN, ERβ selective agonist) administration. The mRNA levels of interleukin(IL)-17A, IL-21 and RORγt and percentages of T helper (Th) 17 cells were up-regulated in the splenocytes of DPN-treated mice. Activated ERβ was found directly binding to IL-17A and IL-21 gene promoters, and also indirectly promoting IL-21 and RORγt gene transcription through interaction with NF-κB. The expressions of co-stimulatory molecules were increased on antigen-presenting cells (APCs) after DPN administration. It suggests that ERβ is the predominant ER subtype responsible for EAT development, and its activation may enhance Th17-type responses through genomic pathways and alteration of APCs' activities.
2.Resveratrol interacts with estrogen receptor-β to inhibit cell replicative growth and enhance stress resistance by upregulating mitochondrial superoxide dismutase.
Robb EL;Stuart JA Free Radic Biol Med. 2011 Apr 1;50(7):821-31. doi: 10.1016/j.freeradbiomed.2010.12.038. Epub 2011 Jan 6.
trans-Resveratrol (RES) is one of a number of dietary polyphenols that have been reported to beneficially affect human physiology. Although numerous studies have attributed this to direct interactions between RES and histone deacetylases, recently the reliability of these results has been questioned. We have shown that the mitochondrial superoxide dismutase (MnSOD) is substantially upregulated in RES-treated cells. Here we explore the mechanisms underlying this, showing that two of RES's more interesting effects, inhibition of replication and enhancement of stress resistance, are mediated by MnSOD upregulation in three cell lines: MRC5 human lung fibroblasts, C2C12 mouse myoblasts, and SHSY5Y human neuroblastoma cells. When small interfering RNA was used to prevent induction of MnSOD expression, the effects of RES on population doubling time of cells in culture, and resistance to cell death after exposure to hydrogen peroxide or paraquat, were abolished. Interestingly, the RES-induced upregulation of MnSOD levels could be prevented by the estrogen receptor antagonist ICI 182780. RES's effects also could be reproduced using estradiol or the estrogen receptor-β agonist diarylpropionitrile, but not using the estrogen receptor-α agonist propylpyrazole triol.
3.17beta-Estradiol modulates vasoconstriction induced by endothelin-1 following trauma-hemorrhage.
Ba ZF;Lu A;Shimizu T;Szalay L;Schwacha MG;Rue LW 3rd;Bland KI;Chaudry IH Am J Physiol Heart Circ Physiol. 2007 Jan;292(1):H245-50.
Although endothelin-1 (ET-1) induces vasoconstriction, it remains unknown whether 17beta-estradiol (E(2)) treatment following trauma-hemorrhage alters these ET-1-induced vasoconstrictive effects. In addition, the role of the specific estrogen receptor (ER) subtypes (ER-alpha and ER-beta) and the endothelium-localized downstream mechanisms of actions of E(2) remain unclear. We hypothesized that E(2) attenuates increased ET-1-induced vasoconstriction following trauma-hemorrhage via an ER-beta-mediated pathway. To study this, aortic rings were isolated from male Sprague-Dawley rats following trauma-hemorrhage with or without E(2) treatment, and alterations in tension were determined in vitro. Dose-response curves to ET-1 were determined, and the vasoactive properties of E(2), propylpyrazole triol (PPT, ER-alpha agonist), and diarylpropionitrile (DPN, ER-beta agonist) were determined. The results showed that trauma-hemorrhage significantly increased ET-1-induced vasoconstriction; however, administration of E(2) normalized ET-1-induced vasoconstriction in trauma-hemorrhage vessels to the sham-operated control level. The ER-beta agonist DPN counteracted ET-1-induced vasoconstriction, whereas the ER-alpha agonist PPT was ineffective.
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