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Merck
CN

U6756

Sigma-Aldrich

U-73122 水合物

powder

别名:

1- [6-[（（17β）-3- Methoxyestra-1，3，5[10]-三烯-17-基）氨基]己基] -1H-吡咯-2，5-二酮

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关于此项目

经验公式（希尔记法）:
C29H40N2O3 · xH2O
CAS Number:
112648-68-7
分子量:
464.64 (anhydrous basis)
MDL编号:
MFCD12910450
UNSPSC代码:
41106300
PubChem化学物质编号:
24278065
NACRES:
NA.77

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方案

≥97.5% (HPLC)

质量水平

100

表单

powder

颜色

off-white

溶解性

ethanol: ~0.7 mg/mL
DMSO: ~0.9 mg/mL
chloroform: ~10 mg/mL
DMSO: ≤2.6 mg/mL (Achieved with heating.)
ethanol: ≤5 mg/mL (Achieved with heating.)
H2O: insoluble

储存温度

room temp

SMILES字符串

O.COc1ccc2C3CC[C@]4(C)[C@H](CCC4C3CCc2c1)NCCCCCCN5C(=O)C=CC5=O

InChI

1S/C29H40N2O3.H2O/c1-29-16-15-23-22-10-8-21(34-2)19-20(22)7-9-24(23)25(29)11-12-26(29)30-17-5-3-4-6-18-31-27(32)13-14-28(31)33;/h8,10,13-14,19,23-26,30H,3-7,9,11-12,15-18H2,1-2H3;1H2/t23-,24-,25+,26+,29+;/m1./s1

InChI key

WCOYJDRCHHGMRK-BDEPKWELSA-N

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相关类别

应用

U-73122 水合物已用于研究磷脂酶C（PLC）信号在调节沙鼠 Reissner′s 膜（RM）中的上皮 Na+通道（ENaC）功能中的作用。U-73122 还用于研究人脐静脉内皮细胞（HUVEC）中的局部钙反应。

生化/生理作用

抑制 PPI 水解成 IP3，导致细胞溶质游离钙的减少。抑制 G蛋白- 磷脂酶C 活化的偶联，同时保持不受 cAMP 产生的影响。

特点和优势

该化合物在受体分类和信号转导手册的磷脂酶C 页面上有重点介绍。想要浏览手册的其他页面， 请单击此处。

制备说明

U-73122 水合物可溶于乙醇（约 0.7 mg/ml或 加热时，≤ 5mg/ml）、氯仿（约 10 mg/ml）和DMSO（约 0.9 mg/ml或加热时，≤ 2.6mg/ml）。U-73122 水合物不溶于水。

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000455133
0000455133
0000445003
0000445003
0000153720

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Wei Fu et al.
Frontiers in endocrinology, 10, 930-930 (2020-02-23)
Plasma levels of PCSK9 are significantly higher in postmenopausal women. Pharmacologically increased estrogen levels have been shown to lower PCSK9 and LDL-C levels in animals and humans. The action of estrogen suggests that it has the ability to prevent PCSK9-mediated
Jae Sung Lee et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(37), 15079-15084 (2013-08-28)
Recruitment of release-competent vesicles during sustained synaptic activity is one of the major factors governing short-term plasticity. During bursts of synaptic activity, vesicles are recruited to a fast-releasing pool from a reluctant vesicle pool through an actin-dependent mechanism. We now
Wagner Shin Nishitani et al.
PloS one, 6(10), e26181-e26181 (2011-11-05)
A new device was designed to generate a localized mechanical vibration of flexible gels where human umbilical vein endothelial cells (HUVECs) were cultured to mechanically stimulate these cells at subcellular locations. A Fluorescence Resonance Energy Transfer (FRET)-based calcium biosensor (an
D I Yule et al.
The Journal of biological chemistry, 267(20), 13830-13835 (1992-07-15)
Stimulation of rat pancreatic acinar cells with low concentrations of phosphatidylinositol (PI)-linked secretagogues induces [Ca2+]i oscillations, without measurable changes in the formation of inositol 1,4,5-trisphosphate. Therefore, we tested U73122 a new phospholipase C inhibitor to determine if PI turnover is
J E Bleasdale et al.
The Journal of pharmacology and experimental therapeutics, 255(2), 756-768 (1990-11-01)
Aggregation of human platelets induced by a variety of agonists was inhibited by 1-[6-[[17 beta-3-methoxyestra-1,3,5(10)-trien-17-yl] amino]hexyl]-1H-pyrrole-2,5-dionel (U-73122) (IC50 values 1-5 microM), but not by the close analog 1-[6-[[17 beta-3-methoxyestra- 1,3,5(10)-trien-17-yl]amino]hexyl]-2,5-pyrrolidine-dione (U-73343) in which pyrrolidinedione was substituted for pyrroledione. Inhibition by
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