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Hypericin(also known as SGX301), is a novel, first-in-class photodynamic therapy using a potent photosensitizer, synthetic hypericin, that is topically applied and activated by safe visible fluorescent light.
| ln Vitro |
The development of melanocytes (Mc), cultured cells (Kc), and cell fibers (Fb) is enhanced by hypericin (0.25–4 μM; 24 h) [2]. Treatment with hypericin (3 μM; 24 h) can cause cell transplantation.
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| ln Vivo |
Treatment with hypericin (intravenous injection; 10 mg/kg; once) slows the growth of tumors [3].
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| Cell Assay |
Cell viability assay [2]
Cell Types: fibroblasts (Fb), melanocytes (Mc) and keratinocytes (Kc). Tested Concentrations: 0.25 μM; [2]. 0.5μM; 1μM; 2μM; 3μM; 4 μM Incubation Duration: 24 hrs (hours) Experimental Results: The LD50 of Fb and Mc were 1.75 μM and 3.5 μM respectively, and the LD50 dose of Kc was greater than 4 μM. Apoptosis analysis[2] Cell Types: Fibroblasts (Fb), Melanocytes (Mc) and Keratinocytes (Kc) Tested Concentrations: 3 μM Incubation Duration: 24 hrs (hours) Experimental Results: Significant (p<0.001) an early apoptotic Fb population (64%), and a smaller, significant (p<0.05) early apoptotic Mc population (20%). |
| Animal Protocol |
Animal/Disease Models: 18-20 week old female balb/c (Bagg ALBino) mouse were injected with CT26 cancer [3]
Doses: 10 mg/kg Route of Administration: intravenous (iv) (iv)injection; 10 mg/kg; Experimental Results:Compared with the control group, tumor growth was delayed Four times. |
| References |
[1]. A Kubin, et al. Hypericin--the facts about a controversial agent. Curr Pharm Des. 2005;11(2):233-53.
[2]. A Popovic, et al. Differential susceptibility of primary cultured human skin cells to hypericin PDT in an in vitro model. J Photochem Photobiol B. 2015 Aug;149:249-56. [3]. Renata Sanovic, et al. Low dose hypericin-PDT induces complete tumor regression in BALB/c mice bearing CT26 colon carcinoma. Photodiagnosis Photodyn Ther. 2011 Dec;8(4):291-6. |
| Molecular Formula |
C30H16O8
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|---|---|
| Molecular Weight |
504.45
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| Exact Mass |
504.0845
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| CAS # |
548-04-9
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| Related CAS # |
Hypericin-d2;Hypericin-d10
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| SMILES |
O([H])C1C2=C(C([H])=C(C3C4C(=C([H])C(=C5C(=C6C(C([H])=C(C([H])([H])[H])C7=C8C(C([H])([H])[H])=C([H])C(C=1C8=C(C=32)C(C=45)=C76)=O)=O)O[H])O[H])O[H])O[H])O[H]
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| Synonyms |
SGX-301 SGX301 SGX 301 NSC 622946 NSC 407313 hypericin.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 : ~250 mg/mL (~495.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.12 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: 2.08 mg/mL (4.12 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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 | 1.9824 mL | 9.9118 mL | 19.8236 mL | |
| 5 mM | 0.3965 mL | 1.9824 mL | 3.9647 mL | |
| 10 mM | 0.1982 mL | 0.9912 mL | 1.9824 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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