DPN

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 50mg
ArtNr HY-12452-50mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
Diarylpropionitrile
CAS No.
1428-67-7
Purity
>98%
MW
2392692
Formula
C15H13NO2
Solubility
10 mM in DMSO
Biological Description
Diarylpropionitrile(DPN) is a non-steroidal estrogen receptor beta(ER beta) selective ligand.
IC50 value:
Target: ER beta ligand
in 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-1beta and IL-6 through attenuation of Abeta1-42-induced phosphorylation of mitogen-activated protein kinases JNK and p38. In addition, DPN enhanced ERK1/2 and Akt phosphorylation depressed by Abeta1-42 [1]. ERbeta was expressed in RAW264.7 cells, and DPN statistically significantly decreased LPS-induced RANTES production in RAW264.7 cells. Small interfering RNA targeting the ERbeta gene inhibited the effect of DPN on RANTES production. In addition, DPN inhibited nuclear translocation and phosphorylation of p65 by inhibiting IkappaB degradation and thus prohibited the activation of nuclear factor kappaB (NF-kappaB) [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 ERbeta CKO mice [2].

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HY-12452-50mg.pdf

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