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| ln Vitro |
It inhibits the conductance of voltage-gated channels (Ca2+, K+, Na+) and ligand-gated channels (GABA, NMDA, and AMPA receptors) [2]. Hypericin dicyclohexylammonium salt (0.1, 1) Hypericin dicyclohexylammonium salt (0.1, 1,10 μM; 2 h) Inhibits TNF-α-stimulated HaCaT (0.1, 1,10 μM; 2 h) Inhibits TNF-α stimulated HaCaT Hypericin dicyclohexylammonium salt (IC50=3.7 μmol/L) Inhibits the formation of HDMEC microvessels and Proliferation is dose-dependent and has no harmful effects [4].]
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| ln Vivo |
Hypericin dicyclohexylammonium salt (5 mg/kg; intraperitoneal injection; once a day for 7 days) can ameliorate the skin lesions of imiquimod-induced silver chip disease and prevent the release of regulatory factors and cytokines[ 3].
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| Cell Assay |
Western Blot Analysis [3]
Cell Types: HaCaT cells Tested Concentrations: 0.1, 1, 10 μM; with or without 10, 20 ng/mL TNF-α Incubation Duration: 2 hrs (hours) Experimental Results: p-p38, p-ERK, p The expression of -JNK and p-STAT3 was diminished, especially at the 10 μM dose. |
| Animal Protocol |
Animal/Disease Models: IMQ - induced psoriasis-like mouse model [3]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 7 days Experimental Results: Skin lesions were Dramatically improved and skin inflammation was Dramatically improved during the entire treatment period This is evidenced by diminished severity scores. Inhibits the infiltration of CD3+ T cells in skin lesions and downregulates the expression of Il1, Il6, Il23, Il17a, Il22, and antimicrobial peptide (AMP). |
| References |
[1]. Heiser JH, et al. TRPC6 channel-mediated neurite outgrowth in PC12 cells and hippocampal neurons involves activation of RAS/MEK/ERK, PI3K, and CAMKIV signaling. J Neurochem. 2013 Nov;127(3):303-13.
[2]. Pochwat B, et al. Hyperforin Potentiates Antidepressant-Like Activity of Lanicemine in Mice. Front Mol Neurosci. 2018 Dec 12;11:456. [3]. Zhang S, et al. Hyperforin Ameliorates Imiquimod-Induced Psoriasis-Like Murine Skin Inflammation by Modulating IL-17A-Producing γδ T Cells. Front Immunol. 2021 May 5;12:635076. [4]. Adam P, et al. Biosynthesis of hyperforin in Hypericum perforatum. J Med Chem. 2002 Oct 10;45(21):4786-93. [5]. Li XX, et al. Hyperforin: A natural lead compound with multiple pharmacological activities. Phytochemistry. 2023 Feb;206:113526. |
| Molecular Formula |
C35H52O4.C12H23N
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|---|---|
| Molecular Weight |
718.1027
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| CAS # |
238074-03-8
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| Related CAS # |
Hyperforin;11079-53-1
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| SMILES |
C/C(=C/CC[C@@]1([C@@H](C/C=C(\C)/C)C[C@@]2(C(=C(C(=O)[C@]1(C2=O)C(C(C)C)=O)C/C=C(\C)/C)O)C/C=C(\C)/C)C)/C.C1CCC(NC2CCCCC2)CC1 |t:14,&1:5,6,13,18|
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~50 mg/mL (~69.63 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.48 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 (3.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3926 mL | 6.9628 mL | 13.9256 mL | |
| 5 mM | 0.2785 mL | 1.3926 mL | 2.7851 mL | |
| 10 mM | 0.1393 mL | 0.6963 mL | 1.3926 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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