Zinc protoporphyrin IX
(Synonyms: 锌原卟啉,ZnPPIX) 目录号 : GC11208
锌原卟啉 IX (ZnPP) 是金属卟啉中的一员，其中血红素铁被锌取代，成为血红素加氧酶 1 (HO-1) 的竞争性抑制剂。
Cas No.:15442-64-5
Sample solution is provided at 25 µL, 10mM.
Zinc protoporphyrin IX (ZnPP) is a member of metalloporphyrins in which the heme iron is replaced by zinc, which becomes a competitive inhibitor of heme oxygenase 1 (HO-1) [1].
Zinc protoporphyrin IX tested presented anti-vesicular stomatitis virus (VSV) activity without photoactivation, with the reduction in viral titer being about 10-fold for 1 μM Zinc protoporphyrin. At 5 μM, Zinc protoporphyrin IX tested were able to completely abolish VSV infectivity. Photoactivation of the porphyrins significantly enhanced their antiviral activities, with 0.1 μM ZnPPIX completely abolishing VSV infectivity [2]. Zinc protoporphyrin IX (ZnPP) (5 μM; 72 hours) causes the fraction of late apoptotic and necrotic cells increasing from 10.9% in controls to 30.4% after 72 h in C-26 cells[3]. Zinc protoporphyrin IX (1.25-40 μM; 48 or 72 hours) exerts cystostatic/cytotoxic effects against human ovarian carcinoma (MDAH2774), human pancreatic adenocarcinoma (Mia PaCa2), human breast carcinoma (MDA-MB231), murine breast carcinoma (EMT6) cell lines [3].
Zinc Protoporphyrin IX (12.5, 25, 50 mg/kg for i.p.; 12.5, 50 mg/kg for p.o. for 7days) exerts dose-dependent antitumor effects manifested by the retardation of tumor growth in BALB/c mice inoculated with C-26 cells [3]. Zinc Protoporphyrin IX (5 and 20 μg/mouse) dose-dependently inhibited tumor growth in LL/2-tumor model mice. Vascular endothealial growth factor concentration in tumors was reduced by Zinc Protoporphyrin IX [4].
References:
[1]. Fang J, Greish K, Qin H, et al. HSP32 (HO-1) inhibitor, copoly (styrene-maleic acid)-zinc protoporphyrin IX, a water-soluble micelle as anticancer agent: In vitro and in vivo anticancer effect[J]. European Journal of Pharmaceutics and Biopharmaceutics, 2012, 81(3): 540-547.
[2]. Cruz-Oliveira C, Almeida A F, Freire J M, et al. Mechanisms of vesicular stomatitis virus inactivation by protoporphyrin IX, zinc-protoporphyrin IX, and mesoporphyrin IX[J]. Antimicrobial agents and chemotherapy, 2017, 61(6): e00053-17.
[3]. Nowis D, Bugajski M, Winiarska M, et al. Zinc protoporphyrin IX, a heme oxygenase-1 inhibitor, demonstrates potent antitumor effects but is unable to potentiate antitumor effects of chemotherapeutics in mice[J]. BMC cancer, 2008, 8(1): 1-12.
[4]. Hirai K, Sasahira T, Ohmori H, et al. Inhibition of heme oxygenase‐1 by zinc protoporphyrin IX reduces tumor growth of LL/2 lung cancer in C57BL mice[J]. International Journal of Cancer, 2007, 120(3): 500-505.
锌原卟啉 IX (ZnPP) 是金属卟啉中的一员,其中血红素铁被锌取代,成为血红素加氧酶 1 (HO-1) 的竞争性抑制剂[1]。\n
经过测试的锌原卟啉 IX 具有抗水疱性口炎病毒 (VSV) 活性,无需光活化,对于 1 μM 原卟啉锌,病毒滴度降低约 10 倍。在 5 μM 时,经过测试的锌原卟啉 IX 能够完全消除 VSV 感染性。卟啉的光活化显着增强了它们的抗病毒活性,0.1 μM ZnPPIX 完全消除了 VSV 感染性[2]。锌原卟啉 IX (ZnPP)（5 μM；72 小时）导致晚期凋亡和坏死细胞的比例从对照中的 10.9% 增加到 72 小时后 C-26 细胞中的 30.4%[3]。锌原卟啉 IX（1.25-40 μM；48 或 72 小时）对人卵巢癌 (MDAH2774)、人胰腺癌 (Mia PaCa2)、人乳腺癌 (MDA-MB231)、鼠类乳腺癌 (EMT6) 具有抑囊/细胞毒性作用细胞系[3].
锌原卟啉 IX（腹腔注射 12.5、25、50 mg/kg；口服 12.5、50 mg/kg,持续 7 天）在接种 C 的 BALB/c 小鼠中发挥剂量依赖性抗肿瘤作用,表现为肿瘤生长迟缓-26 个细胞 [3]。锌原卟啉 IX（5 和 20 μg/小鼠）剂量依赖性地抑制 LL/2 肿瘤模型小鼠的肿瘤生长。 Zinc Protoporphyrin IX降低了肿瘤中血管内皮生长因子的浓度[4]。
经过测试的锌原卟啉 IX 具有抗水疱性口炎病毒 (VSV) 活性,无需光活化,对于 1 μM 原卟啉锌,病毒滴度降低约 10 倍。在 5 μM 时,经过测试的锌原卟啉 IX 能够完全消除 VSV 感染性。卟啉的光活化显着增强了它们的抗病毒活性,0.1 μM ZnPPIX 完全消除了 VSV 感染性[2]。锌原卟啉 IX (ZnPP)（5 μM；72 小时）导致晚期凋亡和坏死细胞的比例从对照中的 10.9% 增加到 72 小时后 C-26 细胞中的 30.4%[3]。锌原卟啉 IX（1.25-40 μM；48 或 72 小时）对人卵巢癌 (MDAH2774)、人胰腺癌 (Mia PaCa2)、人乳腺癌 (MDA-MB231)、鼠类乳腺癌 (EMT6) 具有抑囊/细胞毒性作用细胞系[3].
锌原卟啉 IX（腹腔注射 12.5、25、50 mg/kg；口服 12.5、50 mg/kg,持续 7 天）在接种 C 的 BALB/c 小鼠中发挥剂量依赖性抗肿瘤作用,表现为肿瘤生长迟缓-26 个细胞 [3]。锌原卟啉 IX（5 和 20 μg/小鼠）剂量依赖性地抑制 LL/2 肿瘤模型小鼠的肿瘤生长。 Zinc Protoporphyrin IX降低了肿瘤中血管内皮生长因子的浓度[4]。
| Cell experiment [1]: | |
|
Cell lines |
Human ovarian carcinoma (MDAH2774), human pancreatic adenocarcinoma (Mia PaCa2), human breast carcinoma (MDA-MB231), murine breast carcinoma (EMT6) cell lines. |
|
Preparation Method |
Tumor cells were dispensed into 96-well plates at a concentration of 5×103 cells per well and allowed to attach overnight. The following day investigated agents were added at indicated concentrations. Cells were kept in dark for 48 or 72 h. After the incubation time the cells were rinsed with PBS and stained with 0.5% crystal violet in 2% ethanol for 10 min at room temperature. Plates were washed four times with tap water and the cells were lysed with 1% SDS solution. Absorbance was measured at 595 nm using an enzyme-linked immunosorbent assay reader, equipped with a 595 nm filter. |
|
Reaction Conditions |
0-40 µM for 48, 72 hours |
|
Applications |
Incubation of C-26 cells with Zinc protoporphyrin IX for 48 or 72 h resulted in dose- and time-dependent reduction of cells in G1 phase of the cell cycle. |
| Animal experiment [1]: | |
|
Animal models |
Murine C-26 model |
|
Preparation Method |
For assessment of antitumor activity of Zinc protoporphyrin IX in vivo, exponentially growing C-26 were harvested, re-suspended in PBS medium to the appropriate concentration, and injected at the dose of 1×105 cells per mouse into the footpad of the right hind limb of experimental mice. Tumor cell viability measured by trypan blue exclusion was always above 95%. For in vivo treatment Zinc protoporphyrin IX was dissolved in DMSO and further diluted in 0.9% NaCl to required concentrations. Final DMSO concentration was always less then 0.1%. Zinc protoporphyrin IX was distributed intraperitoneally at doses from 12.5 to 50 mg per kg of body weight or orally at doses from 11 to 22 mg per kg of body weight. Control animals received 0.1% DMSO solution in 0.9% NaCl i.p. or orally. |
|
Dosage form |
12.5 to 50 mg/kg i.p. for 7 days; 11 to 22 mg/kg oral for 7 days |
|
Applications |
HO-1 inhibitor was administered either intraperitoneally (i.p.) or per os and the tumor volume was monitored every second day, starting from day 7 after inoculation of tumor cells. Zinc protoporphyrin IX exerted dose-dependent antitumor effects manifested by the retardation of tumor growth. A statistical significance was reached on days 17 and 19 for Zinc protoporphyrin IX administered at a dose of 25 mg/kg either i.p. or orally. A stronger effect was observed when Zinc protoporphyrin IX was administered i.p. at a dose of 50 mg/kg, where a statistically significant retardation of tumor growth was observed on days 13-19, as compared with controls . |
|
References: [1]: Nowis D, Bugajski M, Winiarska M, et al. Zinc protoporphyrin IX, a heme oxygenase-1 inhibitor, demonstrates potent antitumor effects but is unable to potentiate antitumor effects of chemotherapeutics in mice[J]. BMC cancer, 2008, 8(1): 1-12. |
|
| Cas No. | 15442-64-5 | SDF | |
| 别名 | 锌原卟啉,ZnPPIX | ||
| 化学名 | zinc;3-[18-(2-carboxyethyl)-8,13-bis(ethenyl)-3,7,12,17-tetramethylporphyrin-21,24-diid-2-yl]propanoic acid | ||
| Canonical SMILES | OC(CCC1=C(C)/C([N-]/C1=C\2)=C/C(C(C)=C/3C=C)=NC3=C/C4=N/C(C(C=C)=C4C)=C\C5=C(C)C(CCC(O)=O)=C2[N-]5)=O.[Zn+2] | ||
| 分子式 | C34H32N4O4Zn | 分子量 | 626.03 |
| 溶解度 | DMSO：slightly soluble | 储存条件 | Store at -20°C, sealed storage, away from moisture |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5974 mL | 7.9868 mL | 15.9737 mL |
| 5 mM | 0.3195 mL | 1.5974 mL | 3.1947 mL |
| 10 mM | 0.1597 mL | 0.7987 mL | 1.5974 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
