| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Hyperforin-DCHA primarily targets the transient receptor potential canonical 6 (TRPC6) channel, acting as an activator. It modulates Ca2+ levels by activating these Ca2+-conducting channels. Additionally, it exhibits a multi-directional mechanism of action by blocking the conductance of ligand-gated channels, including GABA, NMDA, and AMPA receptors, as well as voltage-gated channels such as Ca2+, K+, and Na+ channels.
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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].]
In vitro, Hyperforin-DCHA induces cell cycle arrest and apoptosis in chronic myelogenous leukemia (CML) cells. It prevents lipopolysaccharide (LPS)- and substance P-induced release of IL-6 in astrocytoma cells. It also modulates γδ T cells to secrete IL-17α. These activities demonstrate its broad-spectrum cellular effects, including anti-inflammatory and anticancer properties. |
| 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].
In vivo, Hyperforin-DCHA has been shown to suppress the development of croton oil-induced edema in animal models, indicating anti-inflammatory activity. It improves an imiquimod-induced psoriasis-like mouse model. Its diverse pharmacological activities, including antidepressant, antitumor, and antidiabetic effects, have been reported, supporting its potential for various therapeutic applications. |
| Enzyme Assay |
The in vitro binding assay for Hyperforin-DCHA typically involves studying its interaction with the TRPC6 channel. Cell-free systems, such as membrane preparations or liposomes containing reconstituted TRPC6 channels, can be used to measure channel activity via ion flux assays or patch-clamp techniques. Its effects on other channels like GABA, NMDA, and AMPA receptors can be assessed using similar electrophysiological or radioligand binding methods.
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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. In vitro cellular assays for Hyperforin-DCHA are used to evaluate its effects on various cell types. These include assessing apoptosis and cell cycle arrest in CML cell lines, measuring IL-6 release in astrocytoma cells after LPS or substance P stimulation, and evaluating its effects on IL-17α secretion from γδ T cells. These functional assays help elucidate its mechanism of action and cellular targets. |
| 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). In vivo animal studies for Hyperforin-DCHA have been conducted in models of inflammation and skin disease. The compound's anti-inflammatory activity was demonstrated in a croton oil-induced edema model. Its efficacy was also shown in an imiquimod-induced psoriasis-like mouse model, where it improved the disease phenotype. These studies highlight its potential for treating inflammatory and autoimmune conditions. |
| ADME/Pharmacokinetics |
Hyperforin-DCHA is a stable, cell-permeable compound suitable for research applications. As a dicyclohexylammonium salt, it has improved stability and solubility compared to the free acid form of hyperforin. Its pharmacokinetic properties are characteristic of natural products, but detailed parameters such as half-life and bioavailability are not extensively detailed in the available literature. It is typically administered in in vivo studies via injection or oral gavage.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Hyperforin-DCHA are not extensively detailed in the available literature. As a natural product-derived compound with a long history of use in traditional medicine, it is generally considered to have a manageable safety profile. However, comprehensive toxicological studies for the purified salt form are limited. It is intended for research purposes only and is not for human use.
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| References | |
| Additional Infomation |
Hyperforin-DCHA is a valuable research tool for studying TRPC6 channel function and the diverse pharmacological activities of hyperforin. Its multi-target mechanism of action, involving both ion channels and receptors, makes it a compound of interest in neuroscience, oncology, and inflammation research. It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C35H52O4.C12H23N
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| Molecular Weight |
718.1027
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| Exact Mass |
717.57
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| CAS # |
238074-03-8
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| Related CAS # |
Hyperforin;11079-53-1
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| PubChem CID |
46926346
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| Appearance |
White to light yellow solid powder
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| LogP |
12.622
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
52
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| Complexity |
1260
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)C(=O)[C@]12C(=O)C(=C([C@](C1=O)(C[C@@H]([C@@]2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C.C1CCC(CC1)NC2CCCCC2
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| InChi Key |
KJVNMVCMFQAPDM-DNSWOBEMSA-N
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| InChi Code |
InChI=1S/C35H52O4.C12H23N/c1-22(2)13-12-19-33(11)27(16-14-23(3)4)21-34(20-18-25(7)8)30(37)28(17-15-24(5)6)31(38)35(33,32(34)39)29(36)26(9)10;1-3-7-11(8-4-1)13-12-9-5-2-6-10-12/h13-15,18,26-27,37H,12,16-17,19-21H2,1-11H3;11-13H,1-10H2/t27-,33+,34+,35-;/m0./s1
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| Chemical Name |
N-cyclohexylcyclohexanamine;(1R,5R,7S,8R)-4-hydroxy-8-methyl-3,5,7-tris(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-1-(2-methylpropanoyl)bicyclo[3.3.1]non-3-ene-2,9-dione
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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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