Diarylpropionitrile

Research use only, not for human use.

Diarylpropionitrile (DPN) is a non-steroidal estrogen receptor β(ERβ) selective ligand.

Diarylpropionitrile (DPN) is a non-steroidal estrogen receptor β(ERβ) selective ligand, demonstrates the neuroprotective effects against 10 0M Aβ1-42-induced oxidative stress and inflammation in primary rat cortical cell culture; (1-100 nM) significantly decreases 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; decreases the expression levels of IL-1β and IL-6; inhibits medulloblastoma development via anti-proliferative and pro-apototic pathways.(In Vitro):DPN has a 70-fold ERα relative binding affinity selectivity, and it is a full ERα agonist with a 78-fold ERα potency selectivity (EC50=0.85 nM for ERβ; EC50=66 nM for ERα).DPN (10 nM) prevents morphological alterations from Aβ1-42 (10 μM)-induced toxicity in cultured cortical neurons.DPN (0.1-100 nM) decreases ROS levels in a non-dose response manner.DPN (0.1-100 nM) significantly reduces Aβ1-42-stimulated expression of Bax in a non-dose dependent manner.DPN (0.1-100 nM) reduces activated IL-1 levels induced by Aβ1-42 treatment on cultured cortical neurons.DPN (0.1-100 nM) suppresses the Aβ1-42-upregulated phosphorylation of JNK and p38.(In Vivo):DPN (10 μg; s.c.; daily; for 11 days) increases swimming and decreases immobility in the FST, and increases TPH protein expression in the dorsal raphe nucleus (DR) in rat model.

DPN has a 70-fold ERα relative binding affinity selectivity, and it is a full ERα agonist with a 78-fold ERα potency selectivity (EC50=0.85 nM for ERβ; EC50=66 nM for ERα).DPN (10 nM) prevents morphological alterations from Aβ1-42 (10 μM)-induced toxicity in cultured cortical neurons.DPN (0.1-100 nM) decreases ROS levels in a non-dose response manner.DPN (0.1-100 nM) significantly reduces Aβ1-42-stimulated expression of Bax in a non-dose dependent manner.DPN (0.1-100 nM) reduces activated IL-1 levels induced by Aβ1-42 treatment on cultured cortical neurons.DPN (0.1-100 nM) suppresses the Aβ1-42-upregulated phosphorylation of JNK and p38.

DPN (10 μg; s.c.; daily; for 11 days) increases swimming and decreases immobility in the FST, and increases TPH protein expression in the dorsal raphe nucleus (DR) in rat model. Animal Model:Adult Sprague-Dawley female rats (220-250 g), ovariectomized animal modelsDosage:10 μg/rat Administration:Subcutaneous injections, daily, for 11 days Result:Increased swimming and decreased immobility in the FST.

DPN

Endocrinology/Hormones

Estrogen Receptor/ERR

Estrogen Receptor/ERR

Neurological Disease

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1428-67-7

239.2692

C15H13NO2

>98% (HPLC)

10 mM in DMSO

C1=CC(=CC=C1CC(C#N)C2=CC=C(C=C2)O)O

Benzenepropanenitrile, 4-hydroxy-α-(4-hydroxyphenyl)-

(-20℃)

With Ice Pack

≥ 2 years