PRE-084 hydrochloride

Name: PRE-084 hydrochloride
Brand: MedChemExpress
SKU: HY-18100A
Rating: 5.0 (10 reviews)

Cat. No.: HY-18100A Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

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PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC₅₀ of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.

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

PRE-084 hydrochloride Chemical Structure

CAS No. : 75136-54-8

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 83	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 83	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 48	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 75	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 990	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of PRE-084 hydrochloride:

PRE-084 Get quote

8 Publications Citing Use of MCE PRE-084 hydrochloride

: PRE-084 hydrochloride purchased from MedChemExpress. Usage Cited in: Exp Neurol. 2022 Mar 5;114034. [Abstract]; The therapeutic effect of the σ-1R agonist PRE-084 (0.6 mg/kg; i.p.) in SPS rats is blocked by the mTOR signaling pathway inhibitor Rapamycin.

: PRE-084 hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2020 Apr;41(4):499-507. [Abstract]; Chronic PRE-084 treatment alleviates DA neuron loss in Dicer cKO mice. TH and Iba1 immunostaining. Representative photomicrographs are shown at ×20 magnification (scale bars, 100 μm).

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

eNOS	Sigma 1 Receptor

In Vitro

PRE-084 hydrochloride (0.1-100 μM; 24 h) protects cultured cortical neurons against β-amyloid toxicity (maximally neuroprotective at 10 μM) and reduces the levels of proapoptotic protein Bax at 10 μM^[1].

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

Cell Viability Assay^[1]

Cell Line:	Cortical cells (βAP(25-35)-induced neurotoxicity model)
Concentration:	0.1-100 µM
Incubation Time:	24 h
Result:	Reduced neuronal toxicity in a bell shaped-manner and is maximally neuroprotective at 10 µM.

Western Blot Analysis^[1]

Cell Line:	Cortical cells (βAP(25-35)-induced neurotoxicity model)
Concentration:	10 µM
Incubation Time:	24 h
Result:	Reduced the levels of proapoptotic protein Bax in cortical neurons induced by βAP(25-35).

In Vivo

PRE-084 hydrochloride (0.25 mg/kg; i.p.; 3 times a week for 8 weeks) displays beneficial effects on motor performance (improves motor neuron survival, ameliorates paw abnormality and grip strength performance) in wobbler mice, and shows neuroprotective effects (increases the levels of BDNF in the gray matter)^[2].
? PRE-084 hydrochloride (1 mg/kg; i.p.; single) protects the heart by activating the Akt?eNOS pathway in myocardial infarction model^[3].

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

Animal Model:	Wobbler mice (4-week-old)^[2].
Dosage:	0.25 mg/kg
Administration:	Intraperitoneal injection; 3 times a week for 8 weeks.
Result:	Significantly improved ameliorated paw abnormality from week 4, and notably improved paw grip strength at week 5. Reduced the number of reactive astrocytes whereas increased the number of pan-macrophage marker CD68-positive cells and CD206+ cells involved in tissue restoration.

Animal Model:	Adult male Sprague‑Dawley rats (220-250 g; myocardial infarction model)^[3].
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; single.
Result:	Significantly decreased the degree of myocardial apoptosis. Led to significantly increased expression of p‑Akt and p‑eNOS.

Molecular Weight

353.88

Formula

C₁₉H₂₈ClNO₃

CAS No.

75136-54-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1(C2=CC=CC=C2)CCCCC1)OCCN3CCOCC3.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 34 mg/mL (96.08 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 33.33 mg/mL (94.18 mM; ultrasonic and warming and heat to 60°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8258 mL	14.1291 mL	28.2582 mL
5 mM	0.5652 mL	2.8258 mL	5.6516 mL
10 mM	0.2826 mL	1.4129 mL	2.8258 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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: ≥ 2.08 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (252 KB) HNMR (211 KB) LCMS (383 KB)

Handling Instructions (2659 KB)

References

[1]. Marrazzo A, et al. Neuroprotective effects of sigma-1 receptor agonists against beta-amyloid-induced toxicity. Neuroreport. 2005 Aug 1;16(11):1223-6. [Content Brief]

[2]. Peviani M, et al. Neuroprotective effects of the Sigma-1 receptor (S1R) agonist PRE-084, in a mouse model of motor neuron disease not linked to SOD1 mutation. Neurobiol Dis. 2014 Feb;62:218-32. [Content Brief]

[3]. Gao QJ, et al. Sigma-1 Receptor Stimulation with PRE-084 Ameliorates Myocardial Ischemia-Reperfusion Injury in Rats. Chin Med J (Engl). 2018 Mar 5;131(5):539-543. [Content Brief]

[4]. Su TP, et al. Sigma compounds derived from phencyclidine: identification of PRE-084, a new, selective sigma ligand. J Pharmacol Exp Ther. 1991 Nov;259(2):543-50. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.8258 mL	14.1291 mL	28.2582 mL	70.6454 mL
	5 mM	0.5652 mL	2.8258 mL	5.6516 mL	14.1291 mL
	10 mM	0.2826 mL	1.4129 mL	2.8258 mL	7.0645 mL
	15 mM	0.1884 mL	0.9419 mL	1.8839 mL	4.7097 mL
	20 mM	0.1413 mL	0.7065 mL	1.4129 mL	3.5323 mL
	25 mM	0.1130 mL	0.5652 mL	1.1303 mL	2.8258 mL
	30 mM	0.0942 mL	0.4710 mL	0.9419 mL	2.3548 mL
	40 mM	0.0706 mL	0.3532 mL	0.7065 mL	1.7661 mL
	50 mM	0.0565 mL	0.2826 mL	0.5652 mL	1.4129 mL
	60 mM	0.0471 mL	0.2355 mL	0.4710 mL	1.1774 mL
	80 mM	0.0353 mL	0.1766 mL	0.3532 mL	0.8831 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.