Referencia número: HY-12452

DPN

(Synonyms: Diarylpropionitrile)

17 Cited Publications

Revisión del cliente

Based on 17 publication(s) in Google Scholar

DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β (ERβ) selective ligand, with an EC₅₀ of 0.85 nM. DPN has neuroprotective effects in a number of neurological diseases.

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Pureza: 99.66%
No. CAS: 1428-67-7
Fòrmula: C₁₅H₁₃NO₂
Peso molecular:239.27

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

DPN Chemical Structure

No. CAS: 1428-67-7

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (17)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β (ERβ) selective ligand, with an EC₅₀ of 0.85 nM. DPN has neuroprotective effects in a number of neurological diseases^[1]^[2].

IC₅₀ & Target^[1]

ERβ

0.85 nM (EC₅₀)

Ver todos los productos específicos de isoformas Estrogen Receptor/ERR :

Cellular Effect

Cell Line	Type	Value	Description	References
HEC-1	EC₅₀	0.85 nM Compound: rac-5	Agonist activity at ERbeta expressed in human HEC1 cells assessed as transcriptional potency after 24 hrs by luciferase-beta galactosidase reporter gene assay Agonist activity at ERbeta expressed in human HEC1 cells assessed as transcriptional potency after 24 hrs by luciferase-beta galactosidase reporter gene assay	[PMID: 19286283]
HEC-1	EC₅₀	3.3 nM Compound: 1, rac-DPN	Agonist activity at human ERbeta expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay Agonist activity at human ERbeta expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay	[PMID: 22122563]
HEC-1	EC₅₀	304 nM Compound: 1, rac-DPN	Agonist activity at human ERalpha expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay Agonist activity at human ERalpha expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay	[PMID: 22122563]
HEC-1	EC₅₀	66 nM Compound: rac-5	Agonist activity at ERalpha expressed in human HEC1 cells assessed as transcriptional potency after 24 hrs by luciferase-beta galactosidase reporter gene assay Agonist activity at ERalpha expressed in human HEC1 cells assessed as transcriptional potency after 24 hrs by luciferase-beta galactosidase reporter gene assay	[PMID: 19286283]
U2OS	EC₅₀	208 nM Compound: 1, rac-DPN	Agonist activity at human ERalpha expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay Agonist activity at human ERalpha expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay	[PMID: 22122563]
U2OS	EC₅₀	3.7 nM Compound: 1, rac-DPN	Agonist activity at human ERbeta expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay Agonist activity at human ERbeta expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay	[PMID: 22122563]

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)^[1].
DPN (10 nM) prevents morphological alterations from Aβ_1-42 (10 μM)-induced toxicity in cultured cortical neurons^[2].
DPN (0.1-100 nM) decreases ROS levels in a non-dose response manner^[2].
DPN (0.1-100 nM) significantly reduces Aβ_1-42-stimulated expression of Bax in a non-dose dependent manner^[2].
DPN (0.1-100 nM) reduces activated IL-1 levels induced by Aβ_1-42 treatment on cultured cortical neurons^[2].
DPN (0.1-100 nM) suppresses the Aβ_1-42-upregulated phosphorylation of JNK and p38^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Adult Sprague-Dawley female rats (220-250 g), ovariectomized animal models^[3]
Dosage:

10 μg/rat
Administration:

Subcutaneous injections, daily, for 11 days
Result:

Increased swimming and decreased immobility in the FST.

Chemical Information

No. CAS 1428-67-7
Appearance Solid
Peso molecular 239.27
Fòrmula C₁₅H₁₃NO₂
Color White to off-white
SMILES

OC1=CC=C(CC(C#N)C2=CC=C(O)C=C2)C=C1
Synonyms

Diarylpropionitrile
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (17)

All Cell Imaging/StainingHistological Imaging/StainingWBFlow CytometryCell Proliferation/Viability Assay

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Journal Impact Factor

Cell Death Dis

Astrocytic YAP prevents the demyelination through promoting expression of cholesterol synthesis genes in experimental autoimmune encephalomyelitis. [Abstract]

2021 Oct 5;12(10):907. PMID: 34611127
Cell Death Dis

ERβ promotes Aβ degradation via the modulation of autophagy. [Abstract]

2019 Jul 22;10(8):565. PMID: 31332160

DPN purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Jul 22;10(8):565. [Abstract]

Cells were treated with DPN (10 nM), the cytoplasm distribution of endogenous LC3 punctate structures was observed by confocal microscopy in SH-SY5Y cells.

DPN purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Jul 22;10(8):565. [Abstract]

Cells were treated with DPN (10 nM), CQ (10 μM), and DPN plus CQ for 12 h. Cell lysates were analyzed by immunoblotting for LC3-II, SQSTM1, and β-actin protein expression.

DPN purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Jul 22;10(8):565. [Abstract]

Cells were treated with DPN (10 nM) or Aβ_1–42 (5 μM) for 12 h and then added CQ (10 μM) for another 12 h. The MTT assay was used to test cell viability.
J Genet Genomics

ERβ-activated LINC01018 promotes endometriosis development by regulating the CDC25C/CDK1/CyclinB1 pathway. [Abstract]

2024 Jun;51(6):617-629. PMID: 38224945
Transl Psychiatry

Estrogen receptor beta signaling enhances extinction memory recall for heroin-conditioned cues in a sex- and region-specific manner. [Abstract]

2024 Jul 12;14(1):283. PMID: 38997258
Front Immunol

Estrogen Acts Through Estrogen Receptor-β to Promote Mannan-Induced Psoriasis-Like Skin Inflammation. [Abstract]

2022 May 19;13:818173. PMID: 35663991

DPN purchased from MedChemExpress. Usage Cited in: Front Immunol. 2022 May 19;13:818173. [Abstract]

Epidermal thickness decreased after PHTPP treatment but increased after DPN (12 mg/kg, s.c.) injection by H&E-stained.

DPN purchased from MedChemExpress. Usage Cited in: Front Immunol. 2022 May 19;13:818173. [Abstract]

γδ T⁺ cells in the draining lymph nodes from female and male mice, OVX and sham operated mice, DPN (12 mg/kg, s.c.) treated mice with and without mannan application.
Ecotoxicol Environ Saf

Bisphenol A interferes with lncRNA Fhadlos2 and RUNX3 association in adolescent mouse ovary. [Abstract]

2023 Jul 1:259:115060. PMID: 37229876
Eur J Pharmacol

Estradiol reduced 5-HT reuptake by downregulating the gene expression of Plasma Membrane Monoamine Transporter (PMAT, Slc29a4) through estrogen receptor β and the MAPK/ERK signaling pathway. [Abstract]

2022 Jun 5;924:174939. PMID: 35398393
J Clin Endocrinol Metab

Organoid Cultures Derived From Patients With Papillary Thyroid Cancer. [Abstract]

2021 Apr 23;106(5):1410-1426. PMID: 33524147
Molecules

Apigenin Inhibits Histamine-Induced Cervical Cancer Tumor Growth by Regulating Estrogen Receptor Expression. [Abstract]

2020 Apr 23;25(8):1960. PMID: 32340124
Sci Rep

Estrogen regulates duodenal calcium absorption and improves postmenopausal osteoporosis by the effect of ERβ on PMCA1b. [Abstract]

2025 May 8;15(1):16053. PMID: 40341576
J Dairy Sci

ERα-NOS/NO/cGMP/PKG-mTOR/KITL/FOXO3a signaling cascade mediates estrogen-induced primordial follicle activation in goats. [Abstract]

2026 Jan 20:S0022-0302(26)00013-5. PMID: 41570914
J Cell Mol Med

Betulinic Acid Suppresses UBE2T Expression via MAPK/ERK Inhibition to Block FANCI and FANCD2 Monoubiquitination in Glioblastoma. [Abstract]

2026 Jan;30(1):e71000. PMID: 41486508
iScience

Reiterated male-to-female violence disrupts hippocampal estrogen receptor β expression, prompting anxiety-like behavior. [Abstract]

2024 Jul 25;27(9):110585. PMID: 39228787
Appl Biochem Biotechnol

ERα, but not ERβ and GPER, Mediates Estradiol-Induced Secretion of TSH in Mouse Pituitary. [Abstract]

2022 Jun;194(6):2492-2502. PMID: 35138554
Behav Brain Res

Selective estrogen receptor activation prior to global cerebral ischemia in female rats impacts microglial activation and anxiety-like behaviors without effects on CA1 neuronal injury. [Abstract]

2024 Jul 26:470:115094. PMID: 38844057
J Gastrointest Oncol

N-myc downstream-regulated gene 2 promotes the protein stability of estrogen receptor beta via inhibition of ubiquitin-protein ligase E3A to suppress colorectal cancer. [Abstract]

2020 Dec;11(6):1200-1213. PMID: 33456993
J Cancer Ther

Breast Cancer MCF-7 Cell Spheroid Culture for Drug Discovery and Development. [Abstract]

2022 Mar;13(3):117-130. PMID: 36311820

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (417.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.1793 mL

20.8965 mL

41.7931 mL

5 mM

0.8359 mL

4.1793 mL

8.3586 mL

10 mM

0.4179 mL

2.0897 mL

4.1793 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (10.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (10.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (10.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Meyers, M. J., et al. Estrogen Receptor-β Potency-Selective Ligands: Structure−Activity Relationship Studies of Diarylpropionitriles and Their Acetylene and Polar Analogues. Journal of Medicinal Chemistry, 2001. 44(24), 4230–4251. [Content Brief]

[2]. 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. [Content Brief]

[3]. Fuzhong Yang, et al. Physiological dosages of estradiol and diarylpropionitrile decrease depressive behavior and increase tryptophan hydroxylase expression in the dorsal raphe nucleus of rats subjected to the forced swim test. Neuroreport. 2019 Jan 16;30(2):66-70. [Content Brief]

[4]. Sherry A. Said, et al. Effects of long-term dietary administration of estrogen receptor-beta agonist diarylpropionitrile on ovariectomized female ICR (CD-1) mice. GeroScience. 2018 Aug; 40(4): 393–403. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.1793 mL	20.8965 mL	41.7931 mL	104.4827 mL
	5 mM	0.8359 mL	4.1793 mL	8.3586 mL	20.8965 mL
	10 mM	0.4179 mL	2.0897 mL	4.1793 mL	10.4483 mL
	15 mM	0.2786 mL	1.3931 mL	2.7862 mL	6.9655 mL
	20 mM	0.2090 mL	1.0448 mL	2.0897 mL	5.2241 mL
	25 mM	0.1672 mL	0.8359 mL	1.6717 mL	4.1793 mL
	30 mM	0.1393 mL	0.6966 mL	1.3931 mL	3.4828 mL
	40 mM	0.1045 mL	0.5224 mL	1.0448 mL	2.6121 mL
	50 mM	0.0836 mL	0.4179 mL	0.8359 mL	2.0897 mL
	60 mM	0.0697 mL	0.3483 mL	0.6966 mL	1.7414 mL
	80 mM	0.0522 mL	0.2612 mL	0.5224 mL	1.3060 mL
	100 mM	0.0418 mL	0.2090 mL	0.4179 mL	1.0448 mL

DPN

17 Cited Publications

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DPN

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

3D Diverse Fragment Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Publications Citing Use of MedChemExpress (MCE) DPN

Ver todos los productos específicos de isoformas Estrogen Receptor/ERR

Actividad biológica

Chemical Information

Publications (17)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

DPN

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

3D Diverse Fragment Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Publications Citing Use of MedChemExpress (MCE) DPN

Ver todos los productos específicos de isoformas Estrogen Receptor/ERR

Actividad biológica

Chemical Information

Publications (17)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

DPN Related Classifications

HY-12452 Related Classifications