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Merck
CN

SML3970

S1RA

≥98% (HPLC)

别名:

4-{2-[5-Methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine, E 52862, E-52862, E52862, MR 309, MR-309, MR309

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关于此项目

经验公式(希尔记法):
C20H23N3O2
化学文摘社编号:
分子量:
337.42
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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assay

≥98% (HPLC)

form

powder

color

, White to light Brown

solubility

DMSO: 2 mg/mL, clear

storage temp.

room temp

Quality Level

Biochem/physiol Actions

Selective, high-affinity sigma-1 receptor antagonist with antinociceptive efficacy in vivo.



S1RA (E-52862) is a selective, high-affinity sigma-1 receptor antagonist (human/guinea pig σ1 Ki = 17/23.5 nM; σ2 Ki = 9.3 μM/rat, >1 μM/guinea pig). S1RA exerts dose-dependent antinociceptive effects in several neuropathic pain models in mice in vivo (16 - 64 mg/kg i.p.).

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

新产品
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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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José Luis Díaz et al.
Journal of medicinal chemistry, 55(19), 8211-8224 (2012-07-13)
The synthesis and pharmacological activity of a new series of 1-arylpyrazoles as potent σ(1) receptor (σ(1)R) antagonists are reported. The new compounds were evaluated in vitro in human σ(1)R and guinea pig σ(2) receptor (σ(2)R) binding assays. The nature of
L Romero et al.
British journal of pharmacology, 166(8), 2289-2306 (2012-03-13)
The sigma-1 (σ(1) ) receptor is a ligand-regulated molecular chaperone that has been involved in pain, but there is limited understanding of the actions associated with its pharmacological modulation. Indeed, the selectivity and pharmacological properties of σ(1) receptor ligands used
Francisco Rafael Nieto et al.
The journal of pain, 13(11), 1107-1121 (2012-10-16)
Sigma-1 (σ(1)) receptors play a role in different types of pain and in central sensitization mechanisms; however, it is unknown whether they are involved in chemotherapy-induced neuropathic pain. We compared the ability of paclitaxel to induce cold (acetone test) and

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