Cyclo-his-pro-TFA-Cyclo-histidyl-proline-TFA-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECyclo(his-pro) TFACat. No.: HY-101402ACAS No.: 936749-56-3Synonyms: Cyclo(histidyl-proline) TFA; Histidylproline diketopiperazineTFA分式: CHFNO分量: 348.28作靶点: NF-B; Endogenous Metabolite作通路: NF-B; Metabolic Enzyme/Protease储存式: -20C

2、, protect from light, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight, stored under nitrogen)溶解性数据体外实验 H2O : 125 mg/mL (358.91 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.8713 mL 14.3563 mL 28.7125 mL5 mM 0.5743 mL 2.8713 mL 5.7425 mL

3、10 mM 0.2871 mL 1.4356 mL 2.8713 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA)种具有服活性的，结构上与促甲状腺激素释放激素相关的环状肽。Cyclo(his-pro) TFA 可以抑制 NF-B 核积累。Cyclo(his-pro) TFA 可以穿越脑屏障并响多种炎症和应激反应。IC50 & Target NF-B Human Endogenous Metabolite1/2

4、Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA; 50 M; 1-48 hours) increases the nuclear level of Nrf2 andinhibits NF-B nuclear translocation. Cyclo(His-Pro) alone has no effect on nuclear translocation of thesetranscription factors 2.Cyclo(his-pro)

5、TFA (50 M; prior to PQ exposure for 48 hours) abolishes protein nitration that followedparaquat (PQ) exposure and lessenes its functional consequences, as shown by decrease in cell apoptosis,detected by caspase 3 activity and by cytochrome c release 2.Cyclo(his-pro) TFA inhibits NF-B nuclear accumul

6、ation induced by paraquat in rat pheochromocytoma PC12cells via the Nrf2/heme oxygenase-1 pathway 2.Western Blot Analysis 1Cell Line: PC12 cellsConcentration: 50 MIncubation Time: 1, 2, 4, 8, 24, 48 hoursResult: Increased the nuclear level of Nrf2 and inhibited NF-B nuclear translocation.体内研究 Cyclo(

7、his-pro) TFA (Cyclo(histidyl-proline) TFA; 1.8 mg/ear; topical application on the right ear; 30 min priorto TPA) reduces TPA-induced ear oedema confirming that it can exert anti-inflammatory effect 2.Cyclo(his-pro) TFA exerts in vivo anti-inflammatory effects in the central nervous system by down-re

8、gulatinghepatic and cerebral TNF expression thereby counteracting LPS-induced gliosis. Moreover, by up-regulating Bip, Cyclo(his-pro) increases the ER stress sensitivity andtriggers the unfolded protein response toalleviate the ER stress 3.Animal Model: Sixty two/three month-old male C57BL/6 mice (2

9、5-30 g) 2Dosage: 1.8 mg/earAdministration: Topical application on the right ear; 30 min prior to TPAResult: Reduced TPA-induced ear oedema.REFERENCES1. Grottelli S, et al. The Role of Cyclo(His-Pro) in Neurodegeneration. Int J Mol Sci. 2016 Aug 12;17(8). pii: E1332.2. Minelli A, et al. Cyclo(His-Pro

10、) exerts anti-inflammatory effects by modulating NF-B and Nrf2 signalling. Int J Biochem Cell Biol. 2012Mar;44(3):525-35.3. Bellezza I, et al. Neuroinflammation and endoplasmic reticulum stress are coregulated by cyclo(His-Pro) to prevent LPS neurotoxicity.Int J Biochem Cell Biol. 2014 Jun;51:159-69.McePdfHeightCaution: Product has not been fully vali