1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel TRP Channel
  3. Hyperforin

Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Hyperforin dicyclohexylammonium salt) usually boasts enhanced water solubility and stability.

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Hyperforin Chemical Structure

Hyperforin Chemical Structure

CAS No. : 11079-53-1

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Description

Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model[1][2][3][4][5].

IC50 & Target

TRPC6[1]

In Vitro

Hyperforin has a multi-directional mechanism of action. It blocks conductance of ligand-gated (GABA, NMDA, and AMPA receptors) and voltage-gated channels (Ca2+, K+, and Na+)[2].
Hyperforin (0.1, 1, 10 μM; 2 h) reduces the expression and secretion of IL-17A in γδ T cell in vitro cultured murine splenic γδ T cells[3].
Hyperforin (0.1, 1, 10 μM; 2 h) suppresses phosphorylation of MAPK and STAT3 pathways in TNF-α stimulated HaCaT cells[3].
Hyperforin (IC50=3.7 μmol/L) inhibits the microvascular tube formation and proliferation of HDMEC in a dose-dependent manner without toxic effects[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[3]

Cell Line: HaCaT cells
Concentration: 0.1, 1, 10 μM; with or without 10, 20 ng/mL TNF-α
Incubation Time: 2 hours
Result: Reduced the expressions of p-p38, p-ERK, p-JNK, and p-STAT3, especially at the dosage of 10 μM.
In Vivo

Hyperforin (5 mg/kg; i.p.; once daily for 7 d) ameliorates Imiquimod (HY-B0180)-induced psoriatic skin lesion in mice, as well as inhibiting inflammatory cell infiltration and inflammatory cytokines release[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: IMQ-induced psoriasis-like mice model[3]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; once daily for 7 days
Result: Significantly ameliorated skin lesion throughout the treatment period, demonstrated by the reduced 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.
Molecular Weight

536.78

Formula

C35H52O4

CAS No.
SMILES

CC(C)C([C@@]12[C@@](C)([C@H](C[C@](C/C=C(C)/C)(C(C(C/C=C(C)/C)=C2O)=O)C1=O)C/C=C(C)/C)CC/C=C(C)/C)=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Hyperforin
Cat. No.:
HY-116330
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