光溜海绵素C

光溜海绵素C用途

Xestospongin C((-)-Xestospongin C)是一种选择性可逆的肌醇1,4,5-三磷酸受体(IP3R)抑制剂。Xestospongin C作为肌浆/内质网Ca2+ATP酶(SERCA)泵的抑制剂,在体内储存。Xestospongin C以358nm的IC50阻断IP3诱导的小脑微粒体Ca2+释放。Xestospongin C是研究神经元和非神经元细胞中IP3R和Ca2+信号传导的结构和功能的一个有价值的工具[1][2][3]。

光溜海绵素C名称

[ CAS 号 ]:
88903-69-9

[ 中文名 ]:
光溜海绵素C

[ 英文名 ]:
Xestospongin C

[英文别名 ]:

araguspongine E
XESTOSPONGIN
Xestospongine C
XEC
ARGUSPONGINE E
Xestospongin C

光溜海绵素C生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 神经疾病

[ 靶点 ]

IP3R

[体外研究]

应用Aβ1-42(20μM；24小时)前预处理的Xestospongin C(XeC；10μM；Aβ前1小时)显示,与单独使用Aβ的治疗组(18.38%)相比,早期凋亡率(9.87%)显著降低[1]。Xestospongin C(10μM；Aβ前1h)和Aβ1-42(20μM；100s)对Ca2+变化的峰值和平均值具有显著的主要影响,并且在原代培养的海马神经元中具有显著的相互作用[1]。

[体内研究]

Xestospongin C(3μM；泵侧脑室注射四周)改善8个月大的阿尔茨海默病雄性APP/PS1小鼠的去抑制样行为和长期空间记忆缺陷[1]。

[参考文献]

[1]. Wang ZJ, et al. Xestospongin C, a Reversible IP3 Receptor Antagonist, Alleviates the Cognitive and Pathological Impairments in APP/PS1 Mice of Alzheimer's Disease. J Alzheimers Dis. 2019;72(4):1217-1231.

[2]. Gafni J, Munsch JA, Lam TH, Catlin MC, Costa LG, Molinski TF, Pessah IN. Xestospongins: potent membrane permeable blockers of the inositol 1,4,5-trisphosphate receptor. Neuron. 1997 Sep;19(3):723-33. doi: 10.1016/s0896-6273(00)80384-0. PMID: 9331361.

[3]. Castonguay A, et al. Xestospongin C is a potent inhibitor of SERCA at a vertebrate synapse. Cell Calcium. 2002;32(1):39-47.

光溜海绵素C物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
564.7±35.0 °C at 760 mmHg

[ 分子式 ]:
C₂₈H₅₀N₂O₂

[ 分子量 ]:
446.709

[ 闪点 ]:
145.6±23.2 °C

[ 精确质量 ]:
446.387238

[ PSA ]:
24.94000

[ LogP ]:
9.02

[ 外观性状 ]:
灰白色

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.542

[ 储存条件 ]:
-20°C，密闭，干燥

光溜海绵素CMSDS

详细MSDS(安全技术说明书)

光溜海绵素C安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

光溜海绵素C文献

mGluR5 in the nucleus accumbens shell regulates morphine-associated contextual memory through reactive oxygen species signaling.

Addict. Biol. 20 , 927-40, (2015)

Emerging evidence indicates that metabotropic glutamate receptor 5 (mGluR5) critically modulates drug and drug-related behaviors. However, the role of mGluR5 in the opiate-induced contextual memory re...

Aβ and NMDAR activation cause mitochondrial dysfunction involving ER calcium release.

Neurobiol. Aging 36(2) , 680-92, (2015)

Early cognitive deficits in Alzheimer's disease (AD) seem to be correlated to dysregulation of glutamate receptors evoked by amyloid-beta (Aβ) peptide. Aβ interference with the activity of N-methyl-d-...

Intracellular Ca(2+) release from endoplasmic reticulum regulates slow wave currents and pacemaker activity of interstitial cells of Cajal.

Am. J. Physiol. Cell Physiol. 308 , C608-20, (2015)

Interstitial cells of Cajal (ICC) provide pacemaker activity in gastrointestinal muscles that underlies segmental and peristaltic contractions. ICC generate electrical slow waves that are due to large...

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