2. Neuronal Signaling GPCR/G Protein
  3. Sigma Receptor 5-HT Receptor
  4. S1RA hydrochloride

S1RA hydrochloride  (Synonyms: E-52862 hydrochloride)

製品番号: HY-18099A 純度: 99.76%
COA 取扱説明書 Technical Support

S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization.

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S1RA hydrochloride

S1RA hydrochloride 構造式

CAS 番号 : 1265917-14-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 在庫あり
Solution
10 mM * 1 mL in DMSO USD 99 在庫あり
Solid
5 mg $90 在庫あり
10 mg $140 在庫あり
25 mg $280 在庫あり
50 mg $450 在庫あり
100 mg $660 在庫あり
250 mg $990 在庫あり
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

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Based on 3 publication(s) in Google Scholar

Other Forms of S1RA hydrochloride:

S1RA hydrochloride 関連抗体

Top Publications Citing Use of Products

Sigma Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Sigma 1 Receptor Sigma 2 Receptor

5-HT Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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製品説明

S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization[1][2].

IC50 & Target

Sigma 1 Receptor

 

5-HT2B Receptor

 

体外実験

S1RA hydrochloride (0.1-10000 nM) shows high affinity to human and guinea pig σ1Rs with Ki values of 17 and 23.5 nM, respectively[1].
S1RA hydrochloride (0.1-10000 nM) shows affinity to human σ2R with Ki values of 9.3 μM[1].
S1RA hydrochloride shows affinity to human 5-HT2B receptor with a Ki value of 328 nM and an IC50 value of 4.7 μM[1].

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

S1RA hydrochloride 関連抗体
体内実験

S1RA hydrochloride (i.p. 16-80 mg/kg or oral administration 32-128 mg/kg; once) dose-dependently inhibits formalin-induced nociception, capsaicin-induced mechanical hypersensitivity and sciatic nerve injury-induced mechanical and thermal hypersensitivity of mice[1].

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

Animal Model: Male CD1 mice[1]
Dosage: 32, 64, 128 and 160 mg/kg
Administration: Intraperitoneal injection; 32, 64, 128 and 160 mg/kg, once
Result: Reduced the permanence time on the rotating rod in rotarod test.
Animal Model: Male CD1 mice with formalin-evoked nociception[1]
Dosage: 20, 40 and 80 mg/kg
Administration: Intraperitoneal injection; 20, 40 and 80 mg/kg, once
Result: Dose-dependently showed analgesic effect on of formalin-evoked nociceptive behaviours of mice.
Animal Model: Male CD1 mice with capsaicin-induced mechanical hypersensitivity[1]
Dosage: 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration)
Administration: Intraperitoneal injection or oral administration; 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration), once
Result: Dose-dependently reversed capsaicin-induced mechanical hypersensitivity in mice.
臨床実験
分子量

373.88

分子式

C20H24ClN3O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3.[H]Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

DMSO : 100 mg/mL (267.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 16.67 mg/mL (44.59 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6747 mL 13.3733 mL 26.7465 mL
5 mM 0.5349 mL 2.6747 mL 5.3493 mL
10 mM 0.2675 mL 1.3373 mL 2.6747 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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 (6.69 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 (6.69 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 110 mg/mL (294.21 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
純度とドキュメンテーション
参考文献

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.6747 mL 13.3733 mL 26.7465 mL 66.8664 mL
5 mM 0.5349 mL 2.6747 mL 5.3493 mL 13.3733 mL
10 mM 0.2675 mL 1.3373 mL 2.6747 mL 6.6866 mL
15 mM 0.1783 mL 0.8916 mL 1.7831 mL 4.4578 mL
20 mM 0.1337 mL 0.6687 mL 1.3373 mL 3.3433 mL
25 mM 0.1070 mL 0.5349 mL 1.0699 mL 2.6747 mL
30 mM 0.0892 mL 0.4458 mL 0.8916 mL 2.2289 mL
40 mM 0.0669 mL 0.3343 mL 0.6687 mL 1.6717 mL
DMSO 50 mM 0.0535 mL 0.2675 mL 0.5349 mL 1.3373 mL
60 mM 0.0446 mL 0.2229 mL 0.4458 mL 1.1144 mL
80 mM 0.0334 mL 0.1672 mL 0.3343 mL 0.8358 mL
100 mM 0.0267 mL 0.1337 mL 0.2675 mL 0.6687 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.

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S1RA hydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

S1RA1265917-14-3E-52862E52862E 52862Sigma Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorneuropathic painspinal sensitizationguinea pigformalincapsaicinCD1 miceInhibitorinhibitorinhibit

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HY-18099A
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