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Key Documents

U6756

Sigma-Aldrich

U-73122 水合物

powder

同義詞:

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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About This Item

經驗公式(希爾表示法):
C29H40N2O3 · xH2O
CAS號碼:
分子量::
464.64 (anhydrous basis)
MDL號碼:
分類程式碼代碼:
41106300
PubChem物質ID:
NACRES:
NA.77

化驗

≥97.5% (HPLC)

形狀

powder

顏色

off-white

溶解度

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

儲存溫度

room temp

SMILES 字串

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 密鑰

WCOYJDRCHHGMRK-BDEPKWELSA-N

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應用

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。

特點和優勢

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

準備報告

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。

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves


分析證明 (COA)

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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
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
R C Smallridge et al.
Endocrinology, 131(4), 1883-1888 (1992-10-01)
TRH increases cytosolic-free calcium ([Ca2+]i) by activating phospholipase C(PL-C), which induces phosphoinositol hydrolysis, leading to Ca2+ mobilization from inositol trisphosphate (IP3) sensitive stores, and by increasing Ca2+ influx. Increases in [Ca2+]i stimulate PRL secretion. We investigated the effects of U-73122
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

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