662035

U-73122

≥98% (HPLC), solid, agonist-induced phospholipase C activation inhibitor, Calbiochem^®

• 别名: U-73122, 1-[6-((17β-3-Methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl]-1H-pyrrole-2,5-dione
• 经验公式（希尔记法）: C₂₉H₄₀N₂O₃
• CAS号: 112648-68-7
• 分子量: 464.64
• MDL號碼: MFCD00893825
• 分類程式碼代碼: 41121800
• NACRES: NA.77

属性

• 产品名称: U-73122, U-73122, CAS 112648-68-7, inhibits agonist-induced phospholipase C activation (IC50 = 1-2.1 µM) in human platelets and neutrophils.
• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze
• 顏色: off-white
• 溶解度: anhydrous DMSO: 1 mg/mL; chloroform: 3 mg/mL; anhydrous ethanol: 500 μg/mL
• 運輸包裝: ambient
• 儲存溫度: 10-30°C
• SMILES 字串: N5(C(=O)C=CC5=O)CCCCCCN[C@@H]1[C@@]2([C@H]([C@H]3[C@H](CC2)c4c(cc(cc4)OC)CC3)CC1)C
• InChI: 1S/C29H40N2O3/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/t23-,24-,25+,26+,29+/m1/s1
• InChI 密鑰: LUFAORPFSVMJIW-ZRJUGLEFSA-N

说明

一般說明

A potent, selective, and cell-permeable inhibitor C-type phosphatidylinositol-specific phospholipases. Inhibits agonist-induced phospholipase C activation (IC₅₀ = 1-2.1 µM) in human platelets and neutrophils. Inhibits ET-1 and parathyroid hormone-induced Ca²⁺ transients (IC₅₀ = 800 nM and 500 nM, respectively). Also inhibits agonist-induced down-regulation of muscarinic receptors in SK-N-SH neuroblastoma cells. Acts as a potent inhibitor of human polymorphonuclear neutrophil adhesion on biological surfaces (IC₅₀ = 50 nM). Reported to abolish T lymphoma cell invasion into fibroblast monolayers.

生化／生理作用

Cell permeable: yes

Primary Target
Agonist-induced phospholipase C activation

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 1-2.1 µM against agonist-induced phospholipase C activation in human platelets and neutrophils; 800 nM and 500 nM, respectively, against ET-1 and parathyroid hormone-induced Ca2+ transients; 50 nM against human polymorphonuclear neutrophil adhesion

警告

Toxicity: Irritant (B)

準備報告

The use of anhydrous solvents is critical for the solubility of the compound; the presence of moisture in the solvent will lower the solubility of the compound.

重構

Unstable in DMSO and ethanol; reconstitute in anhydrous DMSO or ethanol just prior to use. Following reconstitution in anhydrous chloroform, aliquot into single use volumes, evaporate to dryness under a stream of nitrogen, and freeze (-20°C. Dried aliquots are stable for up to 6 months at -20°C. ); Reconstitute dried aliquots in anhydrous DMSO or anhydrous ethanol just prior to use.

其他說明

Stam, J.C., et al. 1998. EMBO J. 17, 4066.
Smith, R.J., et al. 1996. J. Pharmacol. Exp. Ther.278, 320.
Tatrai, A., et al. 1994. Biochim. Biophys. Acta 1224, 595.
Wang, X.D., et al. 1994. Biochim. Biophys. Acta1223, 101.
Bleasdale, J.E., and Fisher, S.K. 1993. Neuroprotocols: A Companion to Methods in Neurosci. 3, 125.
Wu, H., et al. 1992. Biochemistry31, 3370.
Yule, D.I., and Williams, J.A. 1992. J. Biol. Chem.267, 13830.
Thompson, A.K., et al. 1991. J. Biol. Chem.266, 23856.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 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