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SKF 96365 hydrochloride

现货
Catalog No.
B6616
钙池操纵的钙进入(SOCE)抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 680.00
现货
10mg
¥ 800.00
现货
50mg
¥ 3,200.00
Ship with 10-15 days

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Background

SKF 96365 hydrochloride is an inhibitor of store-operated calcium entry (SOCE). Also, it inhibits transient receptor potential cation channels (TRPCs) and voltage-gated sodium current [1] [2] [3].

Store-operated calcium entry (SOCE) increases cytosolic Ca2+ and induces the entry of extracellular calcium. TRPC channels are divided into store-operated and receptor-operated channels and play a critical role in brain development [1] [2].

SKF 96365 hydrochloride is a SOCE inhibitor. In MPP+ stressed PC12 cells, SKF-96365 (10, 50 μM) significantly prevented nuclear damage, decreased LDH release, increased cell viability and inhibited apoptosis. Also, SKF-96365 inhibited Homer1-mediated endoplasmic reticulum (ER) Ca2+ release and intracellular calcium overload induced by MPP+ injury [1]. In rat ventricular myocytes, SKF-96365 inhibited INa in a frequency-dependent and use-dependent way [3]. In Madin Darby canine kidney (MDCK) cells, SKF 96365 (25-100 μM) induced a robust [Ca2+]i transient in a dose-dependent way [4].

In rats, SKF-96365 significantly inhibited persistent spontaneous nociception induced by melittin and reduced hypersensitivity to both mechanical and thermal stimuli. These results suggested that SKF-96365-sensitive TRPC channels were involved in the processing of melittin-induced hypersensitivity and inflammatory pain [2].

References:
[1].  Chen T, Zhu J, Zhang C, et al. Protective effects of SKF-96365, a non-specific inhibitor of SOCE, against MPP+-induced cytotoxicity in PC12 cells: potential role of Homer1. PLoS One, 2013, 8(1): e55601.
[2].  Ding J, Zhang JR, Wang Y, et al. Effects of a non-selective TRPC channel blocker, SKF-96365, on melittin-induced spontaneous persistent nociception and inflammatory pain hypersensitivity. Neurosci Bull, 2012, 28(2): 173-181.
[3].  Chen KH, Liu H, Yang L, et al. SKF-96365 strongly inhibits voltage-gated sodium current in rat ventricular myocytes. Pflugers Arch, 2015, 467(6): 1227-1236.
[4].  Jan CR, Ho CM, Wu SN, et al. Multiple effects of 1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole hydrochloride (SKF 96365) on Ca2+ signaling in MDCK cells: depletion of thapsigargin-sensitive Ca2+ store followed by capacitative Ca2+ entry, activation of a direct Ca2+ entry, and inhibition of thapsigargin-induced capacitative Ca2+ entry. Naunyn Schmiedebergs Arch Pharmacol, 1999, 359(2): 92-101.

文献引用

1. Wang H, Tian L, et al. "The Osteogenic Niche Is a Calcium Reservoir of Bone Micrometastases and Confers Unexpected Therapeutic Vulnerability." Cancer Cell. 2018 Nov 12;34(5):823-839.e7. PMID:30423299
2. Wang Z, Wang Y, et al. "Transient receptor potential channel 1/4 reduces subarachnoid hemorrhage-induced early brain injury in rats via calcineurin-mediated NMDAR and NFAT dephosphorylation." Sci Rep. 2016 Sep 19;6:33577. PMID:27641617

Chemical Properties

StorageStore at RT
M.Wt402.92
Cas No.130495-35-1
FormulaC22H26N2O3.HCl
Solubility≥40.3mg/mL in DMSO
Chemical Name(S)-1-(2-(4-methoxyphenyl)-2-(3-(4-methoxyphenyl)propoxy)ethyl)-1H-imidazole hydrochloride
SDFDownload SDF
Canonical SMILESCOC1=CC=C(C=C1)[C@@H](CN2C=CN=C2)OCCCC(C=C3)=CC=C3OC.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

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SKF 96365 hydrochloride

相关生物数据

SKF 96365 hydrochloride

相关生物数据

SKF 96365 hydrochloride