JavaScript 似乎在您的浏览器中禁用。 在我们的网站上获得最佳体验，请务必打开 Javascript 在您的浏览器。

为了获得访问"阿拉丁铁蛋"实时聊天框的流畅支持体验，建议您使用Chrome浏览器或选择360浏览器极速模式(如何切换极速模式?)，感谢您选择我们！

切换导航

我的购物车

搜索

S1RA

Sigma 受体拮抗剂

规格或纯度: 98%

CAS编号: 878141-96-9
分子式: C₂₀H₂₃N₃O₂
分子量: 337.42
PubChem编号: 44247568

有货

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭

库存信息

关闭

货号 (SKU)	包装规格	是否现货	价格	数量
S413619-5mg	5mg	现货
S413619-10mg	10mg	现货
S413619-25mg	25mg	现货
S413619-50mg	50mg	期货
S413619-100mg	100mg	现货
S413619-250mg	250mg	现货

查看相关系列

sigma non-opioid intracellular receptor 1 Antagonist

Skip to the end of the images gallery

main product photo

Skip to the beginning of the images gallery

基本描述

英文别名	S1RA\|878141-96-9\|E-52862\|ZW18DSD1H4\|4-(2-((5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yl)oxy)ethyl)morpholine\|UNII-ZW18DSD1H4\|4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine\|CHEMBL2170062\|API-001\|4-(2-(5-Methyl-1-(naphthalen-2-yl)-1H-pyraz
规格或纯度	98%
英文名称	S1RA
生化机理	S1RA (E-52862) is a selective sigma-1 receptor (σ1R) antagonist with a reported binding affinity of Ki = 17.0 ± 7.0 nM for human σ1 receptor , selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels.
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	S1RA (E-52862)是一种选择性sigma-1 receptor (σ1R)拮抗剂，对人源σ1受体的结合亲和力Ki为17 nM。

产品属性

ALogP	3.459
Rotatable Bond	5

名称和标识符

IUPAC Name	4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine
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
InChi Key	DGPGXHRHNRYVDH-UHFFFAOYSA-N
Canonical SMILES	CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4
Isomeric SMILES	CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4
PubChem CID	44247568
分子量	337.42

数据库链接

PubChem CID	44247568
CAS Registry No.	878141-96-9
ChEMBL Ligand	CHEMBL2170062
BindingDB Ligand	50396352
RCSB PDB Ligand	88E

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 67 mg/mL (198.56 mM); Water: 67 mg/mL (198.56 mM); Ethanol: 19 mg/mL (56.3 mM);
DMSO(mg / mL) Max Solubility	67
DMSO(mM) Max Solubility	198.565585916662
Water(mg / mL) Max Solubility	67
Water(mM) Max Solubility	198.565585916662

质检证书(COA)

质检报告(COA)

输入批号以搜索COA:

相关文档

质检报告COA

请输入批号:

SDS中文版 SDS英文版

质量技术规格说明书

可替换产品

产品问答

产品问答

登录提交问题

您提交该产品问题后,我们会在1-2个工作日内给您答复,您可以登录"我的账号",然后点击"我的产品问答"查看答案

参考文献

1. Romero L, Zamanillo D, Nadal X, Sánchez-Arroyos R, Rivera-Arconada I, Dordal A, Montero A, Muro A, Bura A, Segalés C et al.. (2012) Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization.. Br J Pharmacol, 166 (8): (2289-306). [PMID:22404321]
2. Díaz JL, Cuberes R, Berrocal J, Contijoch M, Christmann U, Fernández A, Port A, Holenz J, Buschmann H, Laggner C et al.. (2012) 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, 55 (19): (8211-24). [PMID:22784008]
3. Wünsch B. (2012) The σ(1) receptor antagonist S1RA is a promising candidate for the treatment of neurogenic pain.. J Med Chem, 55 (19): (8209-10). [PMID:22951043]
4. Nieto FR, Cendán CM, Sánchez-Fernández C, Cobos EJ, Entrena JM, Tejada MA, Zamanillo D, Vela JM, Baeyens JM. (2012) Role of sigma-1 receptors in paclitaxel-induced neuropathic pain in mice.. J Pain, 13 (11): (1107-21). [PMID:23063344]
5. Vidal-Torres A, de la Puente B, Rocasalbas M, Touriño C, Bura SA, Fernández-Pastor B, Romero L, Codony X, Zamanillo D, Buschmann H et al.. (2013) Sigma-1 receptor antagonism as opioid adjuvant strategy: enhancement of opioid antinociception without increasing adverse effects.. Eur J Pharmacol, 711 (1-3): (63-72). [PMID:23632394]
6. Sánchez-Fernández C, Montilla-García Á, González-Cano R, Nieto FR, Romero L, Artacho-Cordón A, Montes R, Fernández-Pastor B, Merlos M, Baeyens JM et al.. (2014) Modulation of peripheral μ-opioid analgesia by σ1 receptors.. J Pharmacol Exp Ther, 348 (1): (32-45). [PMID:24155346]
7. Gris G, Merlos M, Vela JM, Zamanillo D, Portillo-Salido E. (2014) S1RA, a selective sigma-1 receptor antagonist, inhibits inflammatory pain in the carrageenan and complete Freund's adjuvant models in mice.. Behav Pharmacol, 25 (3): (226-35). [PMID:24776490]
8. Merlos M, Burgueño J, Portillo-Salido E, Plata-Salamán CR, Vela JM. (2017) Pharmacological Modulation of the Sigma 1 Receptor and the Treatment of Pain.. Adv Exp Med Biol, 964 (13): (85-107). [PMID:28315267]
9. Täubel J, Ferber G, Lorch U, Wang D, Sust M, Camm AJ. (2015) Single Doses up to 800 mg of E-52862 Do Not Prolong the QTc Interval--A Retrospective Validation by Pharmacokinetic-Pharmacodynamic Modelling of Electrocardiography Data Utilising the Effects of a Meal on QTc to Demonstrate ECG Assay Sensitivity.. PLoS ONE, 10 (8): (e0136369). [PMID:26291080]
10. Tejada MA, Montilla-García A, Cronin SJ, Cikes D, Sánchez-Fernández C, González-Cano R, Ruiz-Cantero MC, Penninger JM, Vela JM, Baeyens JM et al.. (2017) Sigma-1 receptors control immune-driven peripheral opioid analgesia during inflammation in mice.. Proc Natl Acad Sci USA, 114 (31): (8396-8401). [PMID:28716934]
11. Bruna J, Videla S, Argyriou AA, Velasco R, Villoria J, Santos C, Nadal C, Cavaletti G, Alberti P, Briani C et al.. (2018) Efficacy of a Novel Sigma-1 Receptor Antagonist for Oxaliplatin-Induced Neuropathy: A Randomized, Double-Blind, Placebo-Controlled Phase IIa Clinical Trial.. Neurotherapeutics, 15 (1): (178-189). [PMID:28924870]
12. Dorsey SG. (2018) Selective Blockade of the Sigma 1 Receptor Has Beneficial Effects on Both Acute and Chronic Oxaliplatin-Induced Peripheral Neuropathy.. Neurotherapeutics, 15 (1): (176-177). [PMID:29110212]
13. Bruna J, Velasco R. (2018) Sigma-1 receptor: a new player in neuroprotection against chemotherapy-induced peripheral neuropathy.. Neural Regen Res, 13 (5): (775-778). [PMID:29862996]
14. Castany S, Codony X, Zamanillo D, Merlos M, Verdú E, Boadas-Vaello P. (2019) Repeated Sigma-1 Receptor Antagonist MR309 Administration Modulates Central Neuropathic Pain Development After Spinal Cord Injury in Mice.. Front Pharmacol, 10 (13): (222). [PMID:30967775]
15. Vidal-Torres A, Fernández-Pastor B, Carceller A, Vela JM, Merlos M, Zamanillo D. (2019) Supraspinal and Peripheral, but Not Intrathecal, σ₁R Blockade by S1RA Enhances Morphine Antinociception.. Front Pharmacol, 10 (13): (422). [PMID:31068818]
16. Carcolé M, Zamanillo D, Merlos M, Fernández-Pastor B, Cabañero D, Maldonado R. (2019) Blockade of the Sigma-1 Receptor Relieves Cognitive and Emotional Impairments Associated to Chronic Osteoarthritis Pain.. Front Pharmacol, 10 (13): (468). [PMID:31130863]

上海阿拉丁生化科技股份有限公司

销售条款及条件隐私政策

© 2016 ALADDIN-E.COM . 版权所有,未经授权禁止拷贝本站资料,如有违反,将追究法律责任

沪公网安备 31012002004058号沪ICP备09093490号-2

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用。

危险品化学品经营许可证（带存储）

营业执照(三证合一)