662035
U-73122
≥98% (HPLC), solid, agonist-induced phospholipase C activation inhibitor, Calbiochem®
別名:
U-73122, 1-[6-((17β-3-Methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl]-1H-pyrrole-2,5-dione
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この商品について
実験式（ヒル表記法）:
C29H40N2O3
CAS番号:
分子量:
464.64
MDL number:
UNSPSC Code:
41121800
NACRES:
NA.77
製品名
U-73122, U-73122, CAS 112648-68-7, inhibits agonist-induced phospholipase C activation (IC50 = 1-2.1 µM) in human platelets and neutrophils.
SMILES string
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 key
LUFAORPFSVMJIW-ZRJUGLEFSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
off-white
solubility
anhydrous DMSO: 1 mg/mL
chloroform: 3 mg/mL
anhydrous ethanol: 500 μg/mL
shipped in
ambient
storage temp.
10-30°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Agonist-induced phospholipase C activation
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
Disclaimer
Toxicity: Irritant (B)
General description
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.
Other Notes
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.
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.
Preparation Note
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
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グローバルトレードアイテム番号
| カタログ番号 | GTIN |
|---|---|
| 662035-5MGCN | 07790788052256 |
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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