| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Hematoporphyrin targets cancer cells in photodynamic therapy applications. Upon light activation, the compound generates reactive oxygen species that selectively destroy tumor cells. The compound is a substrate for affinity chromatography of heme-binding proteins, indicating its interaction with heme-binding proteins.
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| ln Vitro |
Hematoporphyrin (20-120 nM; 60 min) dose-dependently decreases cell survival of U87 and U251 glioma cells with IC50 of 85 and 166 nM, respectively [2]. Hematoporphyrin (85 nM; 60 min) promotes apoptosis by generating ROS in U87 cells [2]. Hematoporphyrin (85 nM; 60 minutes) produces morphological alterations in U87 cells under red light, including shrinkage and fragmentation [2].
In vitro, hematoporphyrin is used in the characterization and synthesis of hematoporphyrin- and hematin-agarose for affinity chromatography of heme-binding proteins. When activated by light, it generates reactive oxygen species that can kill cancer cells in vitro. The compound's photoactivity makes it a valuable tool for studying photodynamic therapy mechanisms. |
| ln Vivo |
In rats exposed to red light radiation, hematoporphyrin (5–10 mg/kg) administered intraperitoneally for two months can significantly reduce tumor size. This is a result of photoactivated porphyrin's direct impact on tumor cells as well as its effects on blood. The ship becomes necrotic as a result of secondary consequences [3].
In vivo, hematoporphyrin has been used in photodynamic therapy for the treatment of certain cancers. When administered to patients and activated by light, the compound generates reactive oxygen species that selectively destroy tumor cells. However, specific in vivo efficacy data are not detailed in the available literature. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for hematoporphyrin typically involve studying its interaction with heme-binding proteins in affinity chromatography applications. The compound is immobilized on agarose beads and used to purify heme-binding proteins from complex mixtures. Binding is assessed by the ability of the matrix to retain specific proteins.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: U87 and U251 Cell Tested Concentrations: 20, 40, 60, 80, 100, 120 nM Incubation Duration: 60 minutes Experimental Results: Inhibition of cell viability in a dose-dependent manner. More effective under red light than white light. Apoptosis analysis [2] Cell Types: U87 Cell Tested Concentrations: 85 nM Incubation Duration: 60 minutes Experimental Results: Apoptotic nuclei were induced in U87 cells at low cell density. Induces ROS and reduces mitochondrial membrane potential. In vitro cell-based assays for hematoporphyrin typically employ cancer cell lines to assess its photodynamic therapy efficacy. Cells are incubated with the compound and then exposed to light at specific wavelengths. Cell viability is assessed by MTT or other standard assays. ROS generation is measured using fluorescent probes. The compound's selective toxicity to tumor cells upon light activation is evaluated. |
| Animal Protocol |
Animal/Disease Models: Hermaphrodite Wistar albino rats (20 days; 60-80 g) with subcutaneoussolid Yoshida hepatoma AH-130 [3]
Doses: 5, 10 mg/kg Route of Administration: Daily intraperitoneal (ip) injection for the first 10 days , followed by intraperitoneal (ip) injections every two weeks for the next 2 months. Experimental Results: After exposing the rats to light for several days, no tumors were palpable. The skin heals completely and the hair grows back. Large areas of coagulative necrosis appeared in the tumor 24 hrs (hrs (hours)) after phototherapy (×40). In vivo animal studies with hematoporphyrin have been conducted in the context of photodynamic therapy research. The compound is administered to tumor-bearing animals, followed by light activation at the tumor site. Tumor regression is monitored, and survival is assessed. However, specific study protocols are not detailed in the available literature. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of hematoporphyrin have been studied in the context of photodynamic therapy. The compound is administered intravenously and accumulates in tumor tissues. It is activated by light at specific wavelengths. Specific PK parameters such as half-life, Cₘₐₓ, and bioavailability have not been detailed in the available literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of hematoporphyrin has been characterized in the context of photodynamic therapy. The compound can cause photosensitivity reactions when patients are exposed to light after administration. No specific toxicology data are available in the provided literature. The compound is intended for research use only.
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| References |
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| Additional Infomation |
Hematoporphyrin is a dicarboxylic acid, a derivative of protoporphyrin in which the vinyl groups at positions 7 and 12 are replaced by 1-hydroxyethyl groups. It is a photosensitizer. It belongs to the protoporphyrin class of compounds and is also a dicarboxylic acid. Functionally, it is related to protoporphyrin. It is an iron-free heme derivative with four methyl groups, two hydroxyethyl groups, and two propionic acid groups attached to its pyrrole ring. Some of these photosensitizers are used in phototherapy for malignant tumors. See also: Hematoporphyrin (note moved to).
Hematoporphyrin is a research-grade porphyrin compound used in photodynamic therapy research and affinity chromatography applications. It is not an approved therapeutic drug in its pure form, though related formulations have been used clinically for PDT. The compound is supplied as a powder with purity >98%. Synonyms include Photodyn and Sensibion. |
| Molecular Formula |
C34H38N4O6
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|---|---|
| Molecular Weight |
598.68872
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| Exact Mass |
598.279
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| CAS # |
14459-29-1
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| Related CAS # |
Hematoporphyrin dihydrochloride;17696-69-4
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| PubChem CID |
11103
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| Appearance |
Pale purple to purple solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
1179.7±65.0 °C at 760 mmHg
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| Melting Point |
172.5°C
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| Flash Point |
667.3±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.642
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| LogP |
5.95
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
44
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KFKRXESVMDBTNQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C34H38N4O6/c1-15-21(7-9-31(41)42)27-14-28-22(8-10-32(43)44)16(2)24(36-28)12-29-34(20(6)40)18(4)26(38-29)13-30-33(19(5)39)17(3)25(37-30)11-23(15)35-27/h11-14,19-20,37-40H,7-10H2,1-6H3,(H,41,42)(H,43,44)
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| Chemical Name |
3-[18-(2-carboxyethyl)-8,13-bis(1-hydroxyethyl)-3,7,12,17-tetramethyl-22,23-dihydroporphyrin-2-yl]propanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~150 mg/mL (~250.55 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.18 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6703 mL | 8.3516 mL | 16.7031 mL | |
| 5 mM | 0.3341 mL | 1.6703 mL | 3.3406 mL | |
| 10 mM | 0.1670 mL | 0.8352 mL | 1.6703 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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