Reagentia en instrumenten voor immunologie, celbiologie en moleculaire biologie.

S1RA [878141-96-9]

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Referentie HY-18099-5mg

Formaat : 5mg

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Telefoonnummer : +1 850 650 7790

Merk : MedChemExpress

Neem contact op met een lokale distributeur :

Telefoonnummer : +1 850 650 7790

S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with K_is of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT_2B receptor (K_i= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice.

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S1RA Chemical Structure

CAS No. : 878141-96-9

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

Other Forms of S1RA:

S1RA hydrochloride In-stock

Voir tous les produits spécifiques à Isoform 5-HT Receptor:

Voir toutes les isoformes

Description

IC₅₀ & Target^[1]^[3]

human σ1R

17 nM (Ki)

guinea pig σ1R

23.5 nM (Ki)

guinea pig σ2R

>1000 nM (Ki)

rat σ2R

9300 nM (Ki)

human 5-HT_2B Receptor

328 nM (Ki)

In Vitro

S1RA (E-52862; 100 µM; 4 h) inhibit intracellular calcium responses in TRPA1 expressing HEK293 cells^[2].
S1RA (100 µM; 4 h) impairs the formation of TRPA1–Sigma-1R complexes and reduces TRPA1 expression at the plasma membrane^[2].

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

In Vivo

S1RA (E-52862; 40 mg/kg; IP; single dose) produces a substantial reduction in pain-related responses to intradermal Allylisothiocyanate (AITC) in WT mice^[2].
S1RA (40 mg/kg; IP; once a day for 11 consecutive days; starting 3 days before Oxaliplatin injection) prevents mechanical and cold hypersensitivity in Oxaliplatin (6 mg/kg; i.p.; Day 0, Day 2, Day 4)-treated mice^[2].

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

Animal Model:	WT and TRPA1 KO mice with AITC (10 µl at 10 mM) in their hind paws^[2]
Dosage:	40 mg/kg
Administration:	IP; single dose; 24-h before evaluation
Result:	Produced a substantial reduction in pain-related responses to intradermal AITC in WT mice.

Masse moléculaire

337.42

Formule

C₂₀H₂₃N₃O₂

CAS No.

878141-96-9

Appearance

Solid

Color

Off-white to yellow

SMILES

CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

1M HCl : 50 mg/mL (148.18 mM; ultrasonic and adjust pH to 1 with HCl)

DMSO : 33.33 mg/mL (98.78 mM; ultrasonic and warming and heat to 60°C; 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	2.9637 mL	14.8183 mL	29.6367 mL
5 mM	0.5927 mL	2.9637 mL	5.9273 mL
10 mM	0.2964 mL	1.4818 mL	2.9637 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité
Calculateur de dilution

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: ≥ 2.5 mg/mL (7.41 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 (7.41 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (7.41 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.

Pureté et documentation

Purity: 99.43%

Select Batch:

Fiche technique (278 KB) SDS (251 KB)

COA (252 KB) HNMR (378 KB) LCMS (129 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Díaz JL, et al. Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862). J Med Chem. 2012 Oct 11;55(19):8211-24. [Content Brief]

[2]. Aida Marcotti, et al. TRPA1 modulation by Sigma-1 receptor prevents oxaliplatin-induced painful peripheral neuropathy. Brain. 2023 Feb 13;146(2):475-491. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO / 1M HCl	1 mM	2.9637 mL	14.8183 mL	29.6367 mL	74.0916 mL
	5 mM	0.5927 mL	2.9637 mL	5.9273 mL	14.8183 mL
	10 mM	0.2964 mL	1.4818 mL	2.9637 mL	7.4092 mL
	15 mM	0.1976 mL	0.9879 mL	1.9758 mL	4.9394 mL
	20 mM	0.1482 mL	0.7409 mL	1.4818 mL	3.7046 mL
	25 mM	0.1185 mL	0.5927 mL	1.1855 mL	2.9637 mL
	30 mM	0.0988 mL	0.4939 mL	0.9879 mL	2.4697 mL
	40 mM	0.0741 mL	0.3705 mL	0.7409 mL	1.8523 mL
	50 mM	0.0593 mL	0.2964 mL	0.5927 mL	1.4818 mL
	60 mM	0.0494 mL	0.2470 mL	0.4939 mL	1.2349 mL
	80 mM	0.0370 mL	0.1852 mL	0.3705 mL	0.9261 mL
1M HCl	100 mM	0.0296 mL	0.1482 mL	0.2964 mL	0.7409 mL

S1RA [878141-96-9]

Referentie HY-18099-5mg

Neem contact op met een lokale distributeur :

Merk : MedChemExpress

Neem contact op met een lokale distributeur :

Other Forms of S1RA:

Voir tous les produits spécifiques à Isoform 5-HT Receptor:

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

S1RA Related Classifications

Keywords:

Misschien heeft u ook interesse in de volgende producten:

S1RA [878141-96-9]

Referentie HY-18099-5mg

Neem contact op met een lokale distributeur :

Merk : MedChemExpress

Neem contact op met een lokale distributeur :

Other Forms of S1RA:

Voir tous les produits spécifiques à Isoform 5-HT Receptor:

S1RA Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

S1RA Related Classifications

Keywords:

Misschien heeft u ook interesse in de volgende producten: