Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
TRPC6[1]
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ln Vitro |
The activity of hyperforin is multidirectional. It inhibits voltage-gated channels (Ca2+, K+, and Na+) as well as ligand-gated channels (GABA, NMDA, and AMPA receptors) in conductance[2]. In vitro-cultured murine splenic γδ T cells demonstrate a reduction in IL-17A expression and secretion upon treatment with hyperforin (0.1, 1, 10 μM; 2 h)[3]. In TNF-stimulated HaCaT cells, hyperforin (0.1, 1, 10 μM; 2 h) inhibits the phosphorylation of the MAPK and STAT3 pathways[3]. Without causing any harmful consequences, hyperforin (IC50=3.7 μmol/L) suppresses the development of microvascular tubes and the proliferation of HDMEC in a dose-dependent manner[4].
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ln Vivo |
Imiquimod psoriatic skin lesions in mice are improved by hyperforin (5 mg/kg; ip; once daily for 7 d); it also prevents inflammatory cell infiltration and the release of inflammatory 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: diminished the expressions of p-p38, p-ERK, p-JNK, and p-STAT3 , especially at the dosage of 10 μM. |
Animal Protocol |
Animal/Disease Models: IMQ-induced psoriasis-like mice model[3]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 7 days Experimental Results: Dramatically ameliorated skin lesion throughout the treatment period, demonstrated by the decreased severity score of skin inflammation. Suppressed infiltration of CD3+ T cells and downregulated expression of Il1 , Il6, Il23, Il17a, Il22, antimicrobial peptides (AMPs) in the skin lesion. |
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
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Molecular Weight |
536.78
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CAS # |
11079-53-1
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Related CAS # |
Hyperforin dicyclohexylammonium salt;238074-03-8
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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)C1(C2=O)C(C(C)C)=O)C/C=C(\C)/C)O)C/C=C(/C)\C)C)/C
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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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8630 mL | 9.3148 mL | 18.6296 mL | |
5 mM | 0.3726 mL | 1.8630 mL | 3.7259 mL | |
10 mM | 0.1863 mL | 0.9315 mL | 1.8630 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.