Teprenone-Geranylgeranylacetone-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETeprenoneCat. No.: HY-B0779CAS No.: 6809-52-5Synonyms: Geranylgeranylacetone分式: CHO分量: 330.55作靶点: HSP作通路: Cell Cycle/DNA Damage; Metabolic Enzyme/Protease储存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month

2、 (stored undernitrogen)溶解性数据体外实验 Ethanol : 50 mg/mL (151.26 mM; Need ultrasonic)DMSO : 5 mg/mL (15.13 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 0.5 mg/mL (1.51 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 0.5 mg/mL (1.51 mM); Clear solution1/3 Master

3、 of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.56 mM); Clear solution4. 请依序添加每种溶剂： 10% EtOH 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.56 mM); Suspended solution; Need ultrasonic5. 请依序添加每种溶剂： 10% EtOH 90% corn oilSolubi

4、lity: 2.5 mg/mL (7.56 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Teprenone种抗溃疡药，为热休克蛋 (heat shock proteins) 的诱导剂。IC50 & Target HSP体外研究 Teprenone is an inducer of HSPs. Teprenone (Geranylgeranylacetone, 1 M) significantly prevents ethanol-induced exfoliation, and reduces lactate dehydrogenase (LDH) re

5、lease in gastric mucosal cells. Teprenone(1 M) gradually increases HSC70 level, and rapidly accumulates the stress-inducible HSP90, HSP70, andHSP60 concentrations within 30-60 min. Teprenone also activates the heat shock factor 1 1. Teprenone (0-20 M) slightly increases human umbilical vein endothel

6、ial cell (HUVEC) viability following irradiation (IR).Teprenone (10 M) exhibits no effects on HUVEC migration and invasion, but enhances HUVEC tubeformation and wound healing both with and without IR. Teprenone (10 M) also promotes angiogenesis byinducing VEGF and eNOS expression in HUVECs 3.体内研究 Te

7、prenone (200 mg/kg, p.o.) results in the accumulation of HSP70 mRNA in rats, and the accumulation isenhanced by stress addition in the mucosa of Teprenone-pretreated rats compared with that of vehicle-pretreated rats. Teprenone (200 mg/kg, p.o.) markedly suppresses the ulcer formation after 2- and 4

8、-hourstress loading in rats 1. Teprenone (200 mg/kg daily) induces HSP72 in retinal ganglion cells (RGCs) fromrat retinas. Teprenone significantly reduces the loss of RGCs (evaluated after intraocular pressure (IOP)elevation), lessens optic nerve damage, decreases the number of TUNEL-positive cells

9、in the RGC layer,and increases HSP72 in a rat model of glaucoma 2. Teprenone (200 mg/kg, p.o.) shows protective effect onradiation-induced intestinal injury in mice 3.PROTOCOLCell Assay 3 Human umbilical vein endothelial cells (HUVECs) are seeded onto 48-well plates at a density of 1 102cells/well b

10、efore Teprenone and/or radiation treatment. Cell viability is determined at 48 h after treatmentusing 0.5 mg/mL MTT solution in serum-free media. This solution is incubated with the cells for 2 h in the37C humidified atmosphere containing 5% CO2. Then, the MTT solution is removed, and the cells ared

11、issolved in 100 L of DMSO. Optical densities of the supernatants are measured at 540 nm with an ELISAspectrophotometer 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Male Wister strain rats weighing approximately 250 g are individually housed

12、in wire-mesh cages in a room2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEAdministration 1 maintained at 23C on a 12-hour light-dark cycle. Rats are allowed free access to a standard laboratorychow. Teprenone (200 mg/kg; as emulsion with 5% gum arabic and 0.008% -tocopherol) or vehicle (5%gum ara

13、bic emulsion containing 0.008% -tocopherol) is given orally in a volume of 5 mL/kg through a metaltubing attached to a 6-mL syringe. Two hours later, rats are placed in restraint cages and then verticallyimmersed in water at 23C to the level of the xyphoid process. The rats are killed by decapitatio

14、n at theindicated times 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Phytother Res. 2018 Jul;32(7):1320-1331.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Hirakawa T, et al. Geranylgeranylacetone induces heat sho

15、ck proteins in cultured guinea pig gastric mucosal cells and rat gastricmucosa. Gastroenterology. 1996 Aug;111(2):345-57.2. Caprioli J, et al. Retinal ganglion cell protection with geranylgeranylacetone, a heat shock protein inducer, in a rat glaucoma model.Trans Am Ophthalmol Soc. 2003;101:39-50; discussion 50-1.3. Han NK, et al. Geranylgeranylacetone Ameliorates Intestinal Radiation Toxicity by Preventing Endothelial Cell Dysfunction.