锌原卟啉作用机制 - Medchemexpress - MCE中国

1、Product Data SheetZinc ProtoporphyrinCat. No.: HY-101193CAS No.: 15442-64-5分式: CHNOZn分量: 626.02作靶点: Reactive Oxygen Species; Endogenous Metabolite; Apoptosis作通路: Immunology/Inflammation; Metabolic Enzyme/Protease; NF-B; Apoptosis储存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 D

2、MSO : 50 mg/mL (79.87 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 1.5974 mL 7.9870 mL 15.9739 mL5 mM 0.3195 mL 1.5974 mL 3.1948 mL10 mM 0.1597 mL 0.7987 mL 1.5974 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -2

3、0C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/m

4、L (3.99 mM); Clear solution此案可获得 2.5 mg/mL (3.99 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (3.99 mM); Suspended solution; Need ultrasonic此案可获得

5、 2.5 mg/mL (3.99 mM) 的均匀悬浊液，悬浊液可于服和腹腔注射。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合BIOLOGICAL ACTIVITY物活性 Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) 种具有服活性的，竞争性的红素加氧酶-1 (HO-1) 抑制剂，显 减弱间苯三酚 (PG) 对 H2O2 的保护作。Zinc Protoporphyrin 可作个体孕妇和童 缺铁的筛查标

6、志物，也于评估群铁状态与红蛋浓度的组合。Zinc Protoporphyrin 具有抗癌活性。IC & Target Human Endogenous Metabolite体外研究Zinc Protoporphyrin (Zn(II)-protoporphyrin IX; 5 M; 72 hours) causes the fraction of late apoptotic and necrotic cellsincreasing from 10.9% in controls to 30.4% after 72 h3.Zinc Protoporphyrin (1.25-40 M; 48 or

7、 72 hours) exerts cystostatic/cytotoxic effects against tumor cells3.Zinc Protoporphyrin (2.5, 5 M; 48 or 72 hours) results in dose- and time-dependent reduction of cells in G1 phase ofthe cell cycle3.Zinc Protoporphyrin (1.25-40 M; 48 hours) leads to accumulation of cleaved (active) caspase-33.Apop

8、tosis Analysis3Cell Line: C-26 cellsConcentration: 5 MIncubation Time: 72 hoursResult: The fraction of late apoptotic and necrotic cells increased from 10.9% in controls to30.4% after 72 h.Cell Cytotoxicity Assay3Cell Line: C-26 and MDA-MB231 cellsConcentration: 1.25, 2.5, 5, 10, 20, 40 MIncubation

9、Time: 48 or 72 hoursResult: Exerted cystostatic/cytotoxic effects against tumor cells.Cell Cycle Analysis3Cell Line: C-26 cellsConcentration: 2.5, 5 MIncubation Time: 48 or 72 hoursResult: Resulted in dose- and time-dependent reduction of cells in G1 phase of the cell cycle.Western Blot Analysis3Cel

10、l Line: C-26 cellsConcentration: 1.25, 2.5, 5, 10, 20, 40 MPage 2 of 3 www.MedChemEIncubation Time: 48 hoursResult: Leaded to accumulation of cleaved (active) caspase-3.体内研究 Zinc Protoporphyrin (12.5, 25, 50 mg/kg for i.p.; 12.5, 50 mg/kg for p.o.; from day 7 to 19) exerts dose-dependentantitumor ef

11、fects manifested by the retardation of tumor growth3.Animal Model: BALB/c mice inoculated with C-26 cells3Dosage: 12.5, 25, 50 mg/kg for i.p.; 12.5, 50 mg/kg for p.o.Administration: IP or PO; from day 7 to 19Result: Exerted dose-dependent antitumor effects manifested by the retardation of tumorgrowt

12、h.REFERENCES1. Park C, et al. Protective Effect of Phloroglucinol on Oxidative Stress-Induced DNA Damage and Apoptosisthrough Activation of the Nrf2/HO-1 SignalingPathway in HaCaT Human Keratinocytes. Mar Drugs. 2019 Apr 13;17(4).2. Mwangi MN, et al. Diagnostic utility of zinc protoporphyrin to dete

13、ct iron deficiency in Kenyan pregnant women. BMC Med. 2014 Nov 26;12:229.3. Nowis D, et al. Zinc protoporphyrin IX, a heme oxygenase-1 inhibitor, demonstrates potent antitumor effects but is unable to potentiate antitumoreffects of chemotherapeutics in mice. BMC Cancer. 2008 Jul 11;8:197.McePdfHeightCaution: Produc