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AB286948

S1RA (E-52862)

S1RA (E-52862)

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(1 Publication)

MW 337.4 Da, Purity >98%. A highly selective sigma-1 receptor antagonist. It shows high affinity for sigma 1 receptors with Ki values of 17 nM and 23.5 nM for human and guinea pig sigma 1 receptors respectively but no significant affinity for the sigma 2 receptors with Ki values of 1000 nM and 9300 nM for guinea pig and rat sigma 2 receptors respectively. It shows moderate affinity (Ki = 328 nM) and antagonistic activity with low potency at the human 5-HT2B receptor. S1RA inhibits neuropathic pain in formalin-induced nociception and capsaicin-induced mechanical hypersensitivity in mice. Sigma receptor modulators may show activity against SARS-CoV-2 as sigma receptors interact with SARS-CoV-2 proteins Nsp6 and Orf9c.

查看别名

5 HT 2B receptor, 5 HT(2B), 5 hydroxytryptamine (serotonin) receptor 2B, 5 hydroxytryptamine (serotonin) receptor 2B G protein coupled, 5 hydroxytryptamine 2B receptor, 5-hydroxytryptamine receptor 2B, 5HT2B_HUMAN, 5HT2F, AL024364, Aging-associated gene 8 protein, Htr 2b, NP75 protein, RP23 167I12.6, SEROTONIN 5HT2B RECEPTOR, SGMR1_HUMAN, SIG-1R, SR-BP, SR31747-binding protein, Serotonin receptor 2B, Sigma 1-type opioid receptor, Sigma non-opioid intracellular receptor 1, Sigma1-receptor, Sigma1R, Sigmar1, Stomach fundus serotonin receptor, hSigmaR1, mSigmaR1, opioid receptor, sigma 1, opioid receptor, sigma 1 isoform 1

关键信息

CAS 号

878141-96-9

纯度

>98%

形式

Solid

form

分子量

337.4 Da

分子式

C<sub>2</sub><sub>0</sub>H<sub>2</sub><sub>3</sub>N<sub>3</sub>O<sub>2</sub>

PubChem

44247568

属性

Synthetic

溶解度

~10 mg/ml in DMF

~1 mg/ml in ethanol

~15 mg/ml in DMSO

生化试剂名称

S1RA

生物学描述

A highly selective sigma-1 receptor antagonist. It shows high affinity for sigma 1 receptors with Ki values of 17 nM and 23.5 nM for human and guinea pig sigma 1 receptors respectively but no significant affinity for the sigma 2 receptors with Ki values of 1000 nM and 9300 nM for guinea pig and rat sigma 2 receptors respectively. It shows moderate affinity (Ki = 328 nM) and antagonistic activity with low potency at the human 5-HT2B receptor. S1RA inhibits neuropathic pain in formalin-induced nociception and capsaicin-induced mechanical hypersensitivity in mice. Sigma receptor modulators may show activity against SARS-CoV-2 as sigma receptors interact with SARS-CoV-2 proteins Nsp6 and Orf9c.

经典 SMILES

CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4

InChi

InChI=1S/C20H23N3O2/c1-16-14-20(25-13-10-22-8-11-24-12-9-22)21-23(16)19-7-6-17-4-2-3-5-18(17)15-19/h2-7,14-15H,8-13H2,1H3

InChiKey

DGPGXHRHNRYVDH-UHFFFAOYSA-N

IUPAC 名

4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine

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搭配使用产品

Assay Kits

AB113850

JC-1 - Mitochondrial Membrane Potential Assay Kit

Functional Studies - JC-1 - Mitochondrial Membrane Potential Assay Kit (AB113850)

  • 4
  • 5
Biochemicals

AB120081

FCCP, mitochondrial oxidative phosphorylation uncoupler

Chemical Structure - FCCP, mitochondrial oxidative phosphorylation uncoupler (AB120081)

  • 4
  • 1
Biochemicals

AB275547

Tetramethylrhodamine, methyl ester (TMRM)

Chemical Structure - Tetramethylrhodamine, methyl ester (TMRM) (AB275547)

  • 0
  • 0
Biochemicals

AB141387

JC-1, Mitochondrial membrane potential dye

Chemical Structure - JC-1, Mitochondrial membrane potential dye (AB141387)

  • 0
  • 0
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产品详情

This product is manufactured by BioVision, an Abcam company and was previously called B3048 S1RA (E-52862). B3048-1 is the same size as the 1 mg size of ab286948.
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性能和储存信息

运输条件
Blue Ice
推荐的短期储存条件
-20°C
推荐的长期储存条件
-20°C
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补充信息

This supplementary information is collated from multiple sources and compiled automatically.

The 5-HT-2B receptor and Sigma1-receptor are two important protein targets with distinct mechanical roles. The 5-HT-2B receptor also known as the serotonin receptor 2B is a G-protein-coupled receptor with an approximate molecular mass of 54 kDa. Sigma1-receptor alternatively sometimes called the sigma-1 receptor is a chaperone protein that acts on multiple subcellular locations with a mass of about 25 kDa. The 5-HT-2B receptor is often expressed in the heart lungs and gastrointestinal tract while the Sigma1-receptor shows expression in the central nervous system liver and kidneys.
Biological function summary

Serotonin receptor 2B influences cardiovascular function gastrointestinal movement and mood regulation through serotonin signaling. It forms a complex with G-proteins to transduce signals. The Sigma1-receptor plays a role in cellular stress response and maintenance of calcium signaling affecting neuroplasticity and cellular survival. It associates with various ion channels and receptors to modulate their functions.

Pathways

Serotonin receptor 2B takes part in the serotonin signaling cascade which is important for mood disorders and vasoconstriction. It interacts closely with other serotonin receptors notably 5-HT-2A and 5-HT-2C in the same family. The Sigma1-receptor participates in neuroprotection pathways by modulating the activity of the ion channels and receptors related to calcium and potassium having impactful interactions with proteins like N-methyl-D-aspartate (NMDA) receptors.

Serotonin receptor 2B is involved in heart valve disease and pulmonary hypertension conditions where improper serotonin signaling can result in pathogenic vascular remodeling. It can influence heart-related disorders through interactions with proteins like transforming growth factor-beta (TGF-beta). The Sigma1-receptor is linked to neurodegenerative disorders such as Alzheimer's disease and amyotrophic lateral sclerosis (ALS) where its modulation of neuronal survival pathways and calcium homeostasis shows a protective effect relating it with markers like amyloid precursor protein (APP) in Alzheimer's pathology.
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产品实验方案

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文献 (1)

Recent publications for all applications. Explore the full list and refine your search

British journal of pharmacology 166:2289-306 PubMed22404321

2012

Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization.

Applications

Unspecified application

Species

Unspecified reactive species

L Romero,D Zamanillo,X Nadal,R Sánchez-Arroyos,I Rivera-Arconada,A Dordal,A Montero,A Muro,A Bura,C Segalés,M Laloya,E Hernández,E Portillo-Salido,M Escriche,X Codony,G Encina,J Burgueño,M Merlos,J M Baeyens,J Giraldo,J A López-García,R Maldonado,C R Plata-Salamán,J M Vela
View all publications
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