DPN (Synonyms: Diarylpropionitrile)

Name: DPN
Brand: MedChemExpress
SKU: HY-12452
Rating: 5.0 (17 reviews)

Cat. No.: HY-12452 Purity: 99.66%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 1428-67-7

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Based on 17 publication(s) in Google Scholar

Other Forms of DPN:

(R)-DPN Get quote
DPN (Standard) Get quote

17 Publications Citing Use of MCE DPN

Cell Imaging/Staining

Histological Imaging/Staining

Flow Cytometry

Cell Proliferation/Viability Assay

: 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.

: 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.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

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.

Molecular Weight

239.27

Formula

C₁₅H₁₃NO₂

CAS No.

1428-67-7

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.66%

Select Batch:

Data Sheet (274 KB) SDS (537 KB)

COA (245 KB) LCMS (403 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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 Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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DPN (Synonyms: Diarylpropionitrile)

Customer Review

Other Forms of DPN:

DPN Related Antibodies

17 Publications Citing Use of MCE DPN

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Estrogen Receptor/ERR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

DPN Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

DPN Related Classifications

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