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Piceatannol(Astringenin NSC-622471 trans-Piceatannol)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Piceatannol(Astringenin NSC-622471 trans-Piceatannol)图片
CAS NO:10083-24-6
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)244.24
FormulaC14H12O4
CAS No.10083-24-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 48 mg/mL (196.5 mM)
Water:<1 mg/mL
Ethanol:<48 mg/mL (196.5 mM)
Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
Synonyms

Synonym: NSC 622471; NSC-622471; Piceatannol; NSC622471.

Chemical Name: (E)-4-[2-(3,5Dihydroxyphenyl)ethenyl]1,2-benzenediol, 3,3′,4,5′-Tetrahydroxy-trans-stilbene

InChi Key: CDRPUGZCRXZLFL-OWOJBTEDSA-N

InChi Code: InChI=1S/C14H12O4/c15-11-5-10(6-12(16)8-11)2-1-9-3-4-13(17)14(18)7-9/h1-8,15-18H/b2-1+

SMILES Code: c1(c(ccc(\C=C\c2cc(O)cc(c2)O)c1)O)O

实验参考方法
In Vitro

In vitro activity: Piceatannol displays ~10-fold selectivity for Syk over Lyn. Piceatannol treatment in RBL-2H3 cells strongly inhibits the antigen-stimulated phosphorylation of Syk and of most other cellular proteins but not the receptor β or γ subunit, in a dose-dependent manner. Piceatannol is also a potent inhibitor of histamine release in mast cells. Selective inhibition of Syk by Piceatannol blocks receptor-mediated down-stream cellular responses in mast cells including prevention of 1,4,5-IP3 synthesis, secretion and membrane ruffling and spreading. Piceatannol also potently inhibits PKA, PKC, MLCK, and CDPK with IC50 of 3 μM, 8 μM, 12 μM, and 19 μM, respectively. Piceatannol selectively prevents the IFNα-induced tyrosine phosphorylation of STAT3 and -5 but not STAT1 and -2, paralleled by the loss of Jak1 and IFNAR1 tyrosine phosphorylation but not Tyk2 and IFNAR2. Piceatannol potently induces apoptotic cell death in BJAB Burkitt-like lymphoma cells with ED50 of 25 μM, through the activation of caspase-3 and mitochondrial permeability transition independent of the CD95/Fas signaling pathway.


Kinase Assay: Recombinant Syk is expressed in baculovirus-infected St9 cells. Assays of recombinant Syk activity are carried out using angiotensin I peptide as substrate. The enzyme activities of recombinant Syk are measured by phosphorylation of angiotensin I peptide in the presence of various concentrations of Piceatannol.


Cell Assay: Cells (LNCaP, DU145, and PC-3) are exposed to increasing concentrations of Piceatannol. For the determination of cell proliferation, cells are assayed at 72 hours by trypan blue exclusion using a hemocytometer. After 1 week, colonies are stained with 1.25% crystal violet and quantified by measuring the absorbance at 595 nm.

In VivoOral administration of Piceatannol induces a remarkable amelioration of the disruption of the colonic architecture, a significant reduction in colonic myeloperoxidase (MPO) activity, and a decrease in production of inflammatory mediators such as nitric oxide (NO), prostaglandin (PG) E2, and pro-inflammatory cytokines in BALB/c mice with dextran sulfate sodium (DSS)-induced colitis. Piceatannol treatment inhibits the rises in blood glucose levels at early stages and improves the impaired glucose tolerance at late stages in type 2 diabetic model db/db mice.
Animal modelFemale BALB/c mice with dextran sulfate sodium (DSS)-induced colitis
Formulation & DosageDissolved in DMSO, and diluted in corn oil;10 mg/kg; oral administration
References

J Biol Chem. 1994 Nov 25;269(47):29697-703.; Int Immunopharmacol. 2008 Dec 10;8(12):1695-702.